Cyclosporine: The Comprehensive Guide
Cyclosporine is a potent immunosuppressant drug derived from a fungus.
It is a revolutionary medicine, most notably by enabling the success of organ transplantation.
Its primary action is to selectively inhibit T-cells, a type of white blood cell that drives the immune response.
Dampening this activity prevents the body’s immune system from attacking and rejecting a transplanted organ.
Beyond transplantation, it is also used to treat severe autoimmune diseases (like psoriasis and rheumatoid arthritis) and certain inflammatory eye conditions.
While highly effective, its use requires careful monitoring due to potential side effects, which can include kidney toxicity, high blood pressure, and increased susceptibility to infections.
What Is Cyclosporine?
Cyclosporine API is a white to off-white crystalline solid with a distinctive skunk-like odor.
It is soluble in acetone, methanol, and water, and it is slightly soluble in water.
It is available in various forms, including soft gels, capsules, oral solutions, injections, and eye drops.
Cyclosporine is a polypeptide composed of eleven amino acids that form a circle; this is where the ‘cyclo’ within cyclosporine originates.
Some people also refer to it as ciclosporine, cyclosporin, or cyclosporin A; they are all the same thing, and these names are interchangeable.
What Is Cyclosporine Used For?
As one of the leading suppliers of cyclosporine in China, we aim to share as much knowledge as possible, enabling pharmaceutical researchers to explore the clinical potential of cyclosporine fully.
It is used for both human medications and the treatment of animal illnesses.
As an anti-rejection medication, it can help a patient live with a foreign organ. It is used during organ and bone marrow transplants to prevent the immune system from rejecting a newly transplanted organ, such as the liver, kidney, or heart.
It can also help reduce inflammation associated with conditions such as ulcerative colitis, rheumatoid arthritis, and atopic dermatitis.
What Is Cyclosporine Used For In Humans?
In humans, cyclosporine is used as an immunosuppressant to prevent organ rejection and to treat certain autoimmune and inflammatory disorders.
You can take it orally as capsules, soft gels, or solutions, or inject it intravenously.
1. Immunosuppressive agents for organ transplant
One of the primary uses of cyclosporine is to prevent organ transplant rejection.
After an organ transplant, the body’s immune system may recognize the transplanted organ as foreign and try to attack it.
Cyclosporine helps to suppress the immune system and reduce the risk of transplant rejection.
Doctors often combine it with other immunosuppressive medications to provide maximal protection against rejection.
Clinically, cyclosporine is an immunosuppressive agent used in transplant patients.
It prevents the rejection of allogeneic kidney, liver, heart, bone marrow, and other organ or tissue transplantation.
Doctors often prescribe tablets or capsules for patients with organ transplants, as they can effectively reduce the activity of the patient’s immune system to lower the risks of organ rejection.
Also, it prevents graft-versus-host reactions in bone marrow transplantation.
2. Treatment of Immune diseases such as rheumatoid arthritis, psoriasis, and Crohn’s (IBD)
It is also used in conjunction with adrenocorticotropic hormone to treat certain immune diseases.
Cyclosporine can manage certain autoimmune and inflammatory disorders, such as rheumatoid arthritis, psoriasis, IBDs such as Crohn’s, ulcerative colitis, etc.
These conditions are characterized by chronic inflammation and overactive immune responses, and cyclosporine helps suppress the immune system and reduce inflammation.
3. Treatment of Eye Diseases
Cyclosporine is also made into ophthalmic solutions/emulsions (eye drops) to treat some ocular diseases, such as dry eye disease (Restasis)
4. Off-Label Uses
Recently, it has been used to treat uveitis, severe aplastic anemia, refractory autoimmune thrombocytopenic purpura, psoriasis, and refractory lupus nephritis, among other conditions.
In addition to these uses, people use it off-label to treat other autoimmune and inflammatory disorders, such as multiple sclerosis and lupus.
What Is Cyclosporine Used For in Dogs?
Its usage for dogs is as follows:
#1. Transplant rejections
Cyclosporine is used to manage transplant rejections in dogs after the operation. It also helps suppress the dog’s immune system from attacking the transplanted organs.
#2. Atopic dermatisis
Atopic dermatitis is a common condition in dogs, characterized by the production of IgE antibodies directed against environmental allergens.
Atopica is not recommended for breeding dogs unless a veterinarian considers the risk-benefit ratio justified.
If you need it to treat your dogs’ atopic dermatitis and the top brands are too expensive, consider finding a local Veterinary clinic that offers compounding to lower your costs.
Even better, if your vet does not have access to raw materials at reasonable prices, you can recommend us, and we will send the samples directly to their clinics on your behalf.
#3. IBD treatment
Cyclosporine is used to treat inflammatory bowel disease (IBD) when immunosuppression is required.
Overall, cyclosporine is a significant player in various immune-related conditions and is expected to remain the primary immunosuppressant in the coming decades.
What are the Cyclosporine Brand Names?
The leading brands of Cyclosporine are Neoral, Gengraf, and Sandimmune.
There is a critical difference between “modified” and “unmodified” formulations, which affects how the drug is absorbed and dosed.
The following table lists the key brands and their characteristics:
| Brand Name | Company | Key Formulation Type |
|---|---|---|
| Neoral | Novartis | Modified (microemulsion) |
| Gengraf | AbbVie | Modified |
| Sandimmune | Novartis | Original (unmodified) |
Understanding Modified vs. Unmodified
This distinction is crucial for patient safety:
Modified Cyclosporine (e.g., Neoral, Gengraf): This is a newer, microemulsion formulation. It provides more consistent and reliable absorption in the body compared to the original form. Most prescriptions today are for this modified type.
Unmodified Cyclosporine (e.g., Sandimmune): The original formulation. Its absorption is less predictable. Notably, Sandimmune oral solution was discontinued in July 2024.
Important Considerations
Do Not Switch Brands: Different brands are not interchangeable without a doctor’s supervision due to the differences in absorption. You should always take the specific brand prescribed and confirm with your pharmacist when filling your prescription.
Other Regional Brands: In some healthcare systems, such as the UK’s NHS, you may also encounter other brand names for the generic (non-branded) version, such as Capimune, Capsorin, or Deximune.
Availability: According to the American Society of Health-System Pharmacists (ASHP), although Sandimmune oral solution has been discontinued, both Neoral and Gengraf oral solutions are currently available on the market.
If you are managing a prescription, it’s best to know your exact brand name and formulation.
If you’re unsure which one you’re taking or have questions about a recent change, please consult your pharmacist or prescribing doctor.
Is Cyclosporine Dangerous?
1. As one of China’s largest suppliers of cyclosporine API, we have received inquiries from several importers about the safety of shipping cyclosporine API by air. We replied with a definite YES!
Cyclosporine (with API purity exceeding 99%) is a common chemical that can be shipped by air or express courier.
We have certificates of safe air transportation from several testing authorities.
2. Someone from Quora is concerned about the overdose of cyclosporine, which is not our specialty; either way, we try to look for more information on the overdose and check out what we have found below.
3. Other customers also worry about its stability during transport at room temperature. They worry that the cyclosporine raw materials may spoil during transit to their warehouse, but we assure them this is unnecessary.
Why?
We have conducted stability tests demonstrating that cyclosporine remains stable for at least 3 years at room temperature and in cold storage within an airplane’s cargo hold.
Now, we will break it down with more data; take a look:
#1. Safety issues of a chemical:
Chemically speaking, the Cyclosporine API powder has been tested and categorized as a safe, common chemical that can be shipped by air or express.
All major shipping companies, including FedEx, TNT, DHL, and UPS, ship packages daily.
It is non-poisonous, and we can tell that by its LD50 value for oral intake:
LD50 in rats by oral is 1480mg/kg
LD50 in mice by oral is 2803mg/kg
LD50 in rabbits by oral is over 1000mg/kg.
LD50 by Intravenous injection:
LD50 for rats by injection is 25mg/kg
LD50 for mice by injection is 107mg/kg
LD50 for rabbits by injection is greater than 10 mg/kg.
It is neither flammable nor explosive.
Its flash point is 736.3°C, and its boiling point is 1293.8°C.
It is relatively stable in heat.
Refer to the MSDS data above for additional safety information on our product page.
#2. Side effects of a drug:
Each drug has side effects, not to mention the fact that you may be overdosing on it.
First, let’s check out its side effects. The damage from overdosing will cause more harm than you think.
1. Nephrotoxicity:
One of its most severe side effects is nephrotoxicity, which might be related to an individual’s susceptibility to it.
It may affect renal function, decrease the glomerular filtration rate, and cause high urine protein, urea nitrogen, and creatinine.
However, in most cases, it is transient and will recover after the drug is reduced and stopped.
However, we recommend that you schedule regular follow-up visits during the medication period, undergo blood tests, and have your liver and kidney function checked.
2. Hypertension:
After taking it, some patients will experience increased blood pressure, which may even induce hypertension.
Therefore, it is essential to monitor this adverse reaction in elderly patients closely.
If you experience symptoms of high blood pressure, it is essential to take your medication carefully and consult your doctor immediately.
3. Cell carcinogenesis:
Like other immunosuppressants, it will significantly increase the possibility of developing lymphoma or other malignant tumors, which means it may cause cancer.
During the period of taking the medication, patients need to avoid excessive exposure to ultraviolet light to prevent malignant skin lesions and incurable skin cancer.
4. Weight gain:
As one of the immunosuppressive drugs, patients may experience weight gain after taking it.
This weight gain occurs because these drugs are prone to water and sodium retention. The body exhibits symptoms of central obesity, which can manifest as a rounded face and slender limbs, but the abdominal muscles become significantly more pronounced.
5. Other side effects:
Other side effects may include increased body hair, gingival hyperplasia, paresthesia, and, in some cases, gastrointestinal disorders.
In severe cases, it may also cause a series of concurrent diseases, such as Raynaud’s syndrome, diabetes, and pancreatitis, and may decrease the number of white blood cells in the blood.
To conclude, it is a common and safe chemical for air shipment; however, it can cause numerous unwanted side effects, so it is advisable to exercise extra caution when taking this medication.
#3. Stability Data as a chemical
As one of the cyclosporine API Manufacturers In China, we must conduct stability tests for all APIs we produce.
Then we provide these stability test data and other documents to the CDE (Center for Drug Evaluation, NMPA).
After our officials approve our drug application and issue an approval number, our APIs can help you develop medicines.
Okay, let’s return to its chemical stability at room temperature.
Cyclosporine is comparatively stable. Assays show it remains stable at room temperature for three to four years.
Any of our customers interested in Stability Data are welcome to contact us.
In summary, cyclosporine is a safe, widely used drug that can be shipped by air. It is not toxic or dangerous.
It has many side effects as a drug, and overdosing can be dangerous.
And it won’t spoil quickly during transportation or storage.
Any customers interested in importing cyclosporine API from China for pharmaceutical manufacturing and compounding are welcome to comment below or contact us directly to explore potential business opportunities.
How Much Does Cyclosporine API Cost In 2025?
For any import, you must first obtain reasonable prices from reliable suppliers. This means extensively sourcing and comparing offers, especially when your budget is limited.
You need to be clear about your budget, how much you can spend, and the quantities you can obtain.
Of course, suppliers have different prices; we provide you with a general export price for your reference.
For commercial orders of 50 kg or more of Cyclosporine API with GMP and FDA approval, the market price from China is approximately USD 1,550 per kilogram, including CNF by air.
For small orders of 1kg, our cost is approximately $USD 2,000~4000 per kilogram (it depends on your quality standard: Chinese GMP/CoPP/CEP, or chemical grade, etc), including door-to-door delivery by express or courier.
If you order only 100~500 Grams, the cost is about 3~4 USD/Gram, including FedEx shipping.
The cost is subject to change due to fluctuations in stock status and raw material prices. Contact us directly for the latest quote.
There has been a shortage of stock from GMP factories in China since October 2021, primarily due to a lack of raw materials.
Only after mid-2022 will the hillock be back.
You can also check the India export prices listed on pharmacompass below:
As you can see from the prices above, the average export price is 1,600 USD per kg, which is similar to ours.
However, we can arrange a fast shipment.
Trust me on the lead time!
We also see that the lowest offer is USD 1350 per kg, which is possible when old stocks need to be sold urgently.
Only in that case would you be able to get prices around 1300 USD.
In other cases, be cautious of potential quality issues at such a low price.
Below are the prices from some reagent companies you may want to look into:
As we can see above, reagent prices are incredibly high and not competitive at all.
They offer discounts to many research institutions due to their long-term business relationships and provide excellent after-sales services.
Either way, it’s up to you to decide where to buy it, depending on your needs.
If you need the chemical urgently, visit the local reagent companies that have it in stock and can ship it promptly.
If your research project is not urgent, you have many other options.
If your order quantities exceed several kilograms, you can consider contacting manufacturers directly for a bulk quote instead of relying on reagent companies.
Who is importing Cyclosporine API From Us?
#1. Our current importers of Cyclosporine API include:
Medicine or Formulation manufacturers
You are in the right place if you are a pharmaceutical manufacturer of finished formulations or medicines.
With our cyclosporine raw materials, you can produce dosage forms such as capsules or tablets.
Our cyclosporine can meet your everyday needs with GMP/DMF for your MOH registration, pilot, and later commercial manufacturing.
Compounding pharmacies
You are in the right spot if you are buying pure cyclosporine API powder for pharmacy compounding.
We have happy pharmacy owners who have been using our materials for over 10 years.
Due to our longstanding relationships, we can request that our regular GMP manufacturer repack orders in quantities less than our standard GMP packaging.
If you contact the GMP manufacturer directly, they may not be willing to accept your repacking from a standard packing unit.
Even if they do, you will probably pay more than the average market price.
As mentioned above, our cyclosporin API is GMP-approved and suitable for manufacturing human dosages.
We can also ensure that all repacking and transportation meet Good Manufacturing Practice (GMP) requirements.
Research institutions
If you are a researcher and need it for research, you can check prices from the local reagent companies listed below.
The best price for it is from TRC-Canada: 65 USD/g for 5g.
Other Sigma and MCE prices are higher.
If you need to message us, we will do our best to deliver first-tier goods at reasonable prices.
You can contact us now for a quote for comparison.
International distributors, traders, and agents
All three types of importers listed above are end users, but that doesn’t mean we don’t work with international distributors or agents. We have many distributors and agents abroad, and we love working with professional distributors.
That’s because not all end users are familiar with import procedures, nor do they want to make the extra effort of importing small quantities of chemicals themselves. Instead, they turn to local suppliers and distributors who are experienced and professional in API imports for help. Thus, there will be no customs issues for end users.
In addition, trading companies are willing to sell quantities below the Minimum Order Quantity set by exporters by repacking standard packages into smaller packages before import.
If your order is too small, the shipping and handling costs may not be worth it, and you can often find better prices from local suppliers and distributors.
Top Manufacturers of Cyclosporine API with GMP in China
NCPC Huasheng Pharmaceutical Co., Ltd
NCPC Huasheng is one of the largest manufacturers of cyclosporine API in China.
Almost half of their cyclosporine API is exported to foreign markets, while the other half is used to manufacture medicines for the domestic Chinese market.
Octagonchem is a designated distributor and supplier of NCPC’s cyclosporine active pharmaceutical ingredient (API). Contact us for our distribution letter.
Zhejiang Ruibang Laboratories
Ruibang is the second-largest manufacturer of cyclosporine APIs in China.
They also manufacture finished cyclosporine capsule formulations for the Chinese domestic market, and unused cyclosporine raw materials are exported to other countries.
Huadong Medicine Co., Ltd
Huadong Medicine, also known as East China Pharma, is the third-largest manufacturer of raw cyclosporine.
Their APIs are primarily designed for high-end markets, such as pharmaceutical manufacturers in the USA and Canada, so their export prices are not particularly competitive.
Other suppliers in China include Joyong Lab, Fujian Kerui Pharma, and Guangdong Taisende, among others.
Besides suppliers in China, there are also foreign suppliers outside of China for it; these competitors include:
1. TEVA CZECH INDUSTRIES S.R.O. Opava CZ
2. AbbVie Inc., North Chicago, US
3. Apotex Fermentation Inc., Winnipeg, CA
4. CKD BIO CORPORATION
5. CURIA ITALY S.R.L. Rozzano, Milano IT
6. CONCORD BIOTECH LIMITED Ahmedabad, IN
The suppliers mentioned above are almost all market players in the cyclosporine API market.
To obtain the best prices for your imports, contact each supplier individually to request a quotation. Then, select the best offer and place your order.
What Is HS Code Of Cyclosporine?
The HS Code classifies goods for Customs purposes, enabling Customs to regulate imports and exports better.
This code will inform you of your import tax rate, whether there are mandatory customs regulations for commodity inspections, and other relevant details.
However, countries use different HS Codes due to differing categorization methods, yet some similarities remain.
If you are not sure, consult your import broker to be on the safe side.
#1 HS Code As an API
Its pure powder is an organic compound and a cyclic peptide composed of 11 amino acids.
Though it is an immunosuppressant, it was classified in China before October 2020 as part of a group of chemical compounds called other antibiotics with HS code 2941909099.
Later, it was categorized as other organic compounds with HS Code 2942000000.
Regarding 29420000, please note that the HS Code starts with 2942. It is tricky, and Chinese Customs are very strict and sensitive.
We declared our Propylthiouracil API powder under HS code 2942000000 (the correct HS code for propylthiouracil is 2933599099).
Customs immediately rejected our export declaration papers due to our false Harmonized System (HS) declaration.
Later, we had to file redeclaration papers to get it released for export from Shanghai airport.
However, some websites claim that the latest HS Code for cyclosporine powder is 2933990099, categorized as Other heterocyclic compounds containing only nitrogen heteroatoms. (其他仅含氮杂原子的杂环化合物)
However, there are also websites considering its HS Code as 2941909099, which is OTHER ANTIBIOTICS (其他抗菌素)
Please note that the latest update on the correct HS code, as of March 2023, is 2941909099.
Ensure your import broker understands the details correctly before your import to avoid delays in Customs Clearance.
#2 HS Code As Finished Formulations (Extra Knowledge for Free)
If you are importing finished formulations, the HS code should be 3004909099, which means ‘Other medicines in prescribed doses’ (其他已配定剂量的药品).
What import permits are needed to import Cyclosporine API?
Regardless of the country where the importer is located, pharmaceutical products pose the most complex issue.
Almost 99% of the pharmaceutical raw materials imported are regulated by the FDA so that you will require authorizations or import permits.
This import permit is the most important thing. Without it, your goods will rot in Customs, and you will have to pay Customs storage fees and destroy them.
Take Egypt, for example. For example, a medicine manufacturer must import Cyclosporine API to manufacture medicine in Egypt.
If the medicine manufacturer plans to import cyclosporine API into Egypt, the importer must apply for an import permit from the Egyptian Ministry of Health.
The documents needed to apply for an import permit are as follows:
1. GMP (CoPP/CEP/WC/TGA, etc., as long as it is approved for import in developed countries, it is all fine)
2. DMF (open and closed part)
Once the required documents for the import permits are approved, the importer will receive the MOH license, which will facilitate clearance with Egyptian Customs.
This is similar for importers in other countries, such as the USA.
Pharmaceutical manufacturers must register with the US FDA to obtain a CDN number for pharmaceutical products imported in commercial quantities.
Additionally, they must submit a DMF, which is later required to obtain CoPP, ultimately leading to a GMP certificate for specific active pharmaceutical ingredients (APIs).
With all that said, you need to ensure you have the permits to import this API.
For research scholars, it should be easier than for human use.
For example, some universities have import permits to import a wide range of APIs and reagents.
Once the chemicals or reagents are in Customs, show the import permits to FedEx. FedEx staff will assist with clearance and can even perform pre-clearance to expedite the process.
How To Ship Cyclosporine API From China To Your Country?
#1. Certification for the safe transport of chemical goods
For chemicals shipped by air, the shipping companies must verify that the chemical is not hazardous and obtain a certificate from the relevant authorities confirming this.
DGM and SICIT (Shanghai Institute of Chemical Industry Testing Co., Ltd.) are the leading authorities for this certification.
The DGM certificate is typically good for South and North China Customs Officials.
The SICIT certificate is not usable in North China for unknown reasons.
If you plan to import bulk cyclosporine API from suppliers in South China, please remind them to apply for DGM certificates to avoid any Customs delays.
In addition to this safety-proof certificate, common Export Declaration Documents for Customs include Commercial Invoices, Packing Lists, Product Descriptions, and Customs Declaration Forms.
As one of the leading suppliers of Cyclosporine API in China, we have been exporting it to customers year-round for over a decade.
After we determine the necessary certificate for air shipping, we will proceed with the shipping options for importing cyclosporine.
#2. Shipping methods
Cyclosporine API powder is a very stable and safe chemical. It is neither poisonous nor dangerous, nor is it flammable, explosive, or oxidizing.
#2.1 By air or courier for small-quantity orders.
For small orders under 10 kg, couriers are the most suitable option.
We recommend shipping them by direct flight to your airport or express courier for urgent orders.
#2.2 By air for an order quantity between 10~100kg
For those quantities, shipping by courier will cost more than air shipping.
So shipping by air is recommended.
#2.3. By sea for Commercial orders over 500kg.
If your order quantity exceeds 500kg, consider shipping it by sea to save on shipping costs.
However, in our experience, the most common method is by air.
Due to its high value, air freight cost is only a tiny part of the total cost.
Air shipping costs about 15 USD per kilo, which is only 1/120 of the price of cyclosporine, so it is never a bad idea to ship your expensive products by air.
#3. Temperature control during transport
During transport, there is no need to ship it with an ice pack to keep it cool, as the powder is stable at room temperature.
#4. Storage
Cyclosporine API should be stored in a dry, cool place, with the inner package sealed well. It should be protected from light and heat to avoid severe temperature fluctuations.
Also, ensure the storage temperature remains stable and does not exceed 25 degrees.
If you store a reference standard, keep it in a refrigerator at a temperature of at least 20 degrees below 0 degrees Celsius.
Any customers interested in importing cyclosporine APIs from China are welcome to contact us for a quote.
If you don’t have a reliable supplier, comment below or email us directly for a quick quotation.
What Is The Shipping Cost Of Cyclosporine API By Air?
Once you have obtained the import permits and identified a suitable cyclosporine supplier in China for your order, consider the shipping methods.
As cyclosporine is not inexpensive, a commercial order over 200kg will be considered significant.
It leaves you with almost one option: to ship it by air or courier.
The general cost per kilogram for orders over 100 kg is approximately USD 1,600, depending on the destination country.
If the destination is far from China, or the country is at war or under sanctions, shipping costs will be higher.
The shipping cost for 100 kg to the USA is approximately $12–$17 USD/kg, and to Europe, it is around $14–$19 USD/kg.
If you order only 1kg or less and still need it shipped to your airport, the shipping cost is approximately $500- $700 per 1kg, which is not worth the expense.
If you can accept FedEx shipping, the starting 500 g is approximately $6,070, and shipping to Europe is around $7,080.
To conclude the whole process:
First, you need to know all the costs associated with the import, as well as the import regulations, and then you’ll be ready to proceed.
This post covers almost everything you need to know about importing Cyclosporine API from China into your country.
If anything is unclear or you have different opinions or better ideas, please comment below or contact us directly.
Compounding Pharmacy Guidelines for Cyclosporine Formulations
Veterinary Use:
Follow USP <795> for extemporaneous compounding.
Use preservatives (e.g., benzalkonium chloride) for ocular formulations.
Human Use:
Avoid diluting Neoral capsules; use approved vehicles.
Label clearly for “transplant” vs. “dermatology” use.
Regulatory Compliance:
State-specific pharmacy board approvals are required.
Document all compounding processes for audits.
Other FAQs About Cyclosporine
When Was Cyclosporine Approved?
There are two primary dosage forms of cyclosporine on the market: oral cyclosporine solution, cyclosporine capsules, and cyclosporine-modified capsules.
The cyclosporine oral solution was approved in 1983, and the cyclosporine capsule was approved in 1990, seven years later.
Cyclosporine-modified capsules and solutions were not approved until 1995.
Over time, more companies launched cyclosporine formulations under their own brands.
However, due to its poor water solubility, cyclosporine dosage forms were limited to capsules and solutions.
Is Cyclosporine A Biologic?
No, it isn’t.
Cyclosporine A is not classified as a biological drug. It is a small-molecule immunosuppressant.
Here’s the distinction:
Biologics are typically large, complex molecules derived from living organisms, such as proteins, antibodies, or genes. They are produced using biotechnology (e.g., recombinant DNA technology). Examples include adalimumab (Humira) and etanercept (Enbrel).
Cyclosporine A is a small-molecule drug originally isolated from a fungus. It works by inhibiting calcineurin, a key enzyme in the immune system, and is used to prevent organ transplant rejection and treat autoimmune diseases.
While it is used for similar purposes as some biologics (e.g., immunosuppression), cyclosporine A is chemically synthesized and not derived from living organisms; thus, it is not a biologic.
Is Cyclosporine A Steroid?
No, it isn’t.
A steroid is a chemical class of hormones. Hormones can be naturally occurring in our bodies or synthesized in laboratories.
A 17-atom, 4-ring structure characterizes all steroids, as seen in spironolactone, hydrocortisone succinate sodium, alpha-estradiol, and 2-methoxyestradiol, among others. You can check their chemical structures to compare with the ring above.
However, cyclosporine’s chemical structure doesn’t have the characteristic 17-atom 4-ring structure; it is a one-ring peptide formed by several amino acids.
Is Cyclosporine An Antibiotic?
No, cyclosporine is not an antibiotic.
Although its name may sound similar to some antibiotics (such as cycloheximide), cyclosporine is an immunosuppressant drug.
- Class: Immunosuppressant (specifically a calcineurin inhibitor)
- Source: Originally derived from the fungus Tolypocladium inflatum
- Function: It suppresses the immune system by inhibiting calcineurin, a protein involved in T-cell activation
- Uses:
- Preventing organ transplant rejection
- Treating autoimmune diseases like rheumatoid arthritis, psoriasis, and nephrotic syndrome
However, it doesn’t count as an antibiotic or belong to any specific antibiotic generation because it doesn’t kill germs or bacteria; instead, it suppresses the immune system.
Why It’s Not an Antibiotic
- Antibiotics are drugs that kill or inhibit the growth of bacteria.
- Cyclosporine does not have antibacterial properties; it targets the immune system, not bacteria or other microorganisms.
So, while cyclosporine is a powerful medication with important medical uses, it is not an antibiotic but rather an immunosuppressant.
Is Cyclosporine The Same As Restasis?
No, it isn’t.
Cyclosporine API is a fine white powder, the active pharmaceutical ingredient in Restasis, while cyclosporine is the generic name.
Restasis is the brand name for AbbVie’s finished formulation of cyclosporine ophthalmic emulsion (0.05%), used to treat chronic dry eye disease.
Restasis contains (Active ingredient: cyclosporine 0.05%, inactive ingredients: glycerin; castor oil; polysorbate 80; carbomer copolymer type A; purified water; and sodium hydroxide)
As we can see, cyclosporine is the generic name, not the brand name Restasis.
When we discuss Restasis for treating a disease, we are referring to cyclosporine as a potential treatment.
However, when we speak of cyclosporine, it doesn’t necessarily mean we want Restasis; it could be other cyclosporine-containing brands.
Generic Cyclosporine vs. Restasis: Key Differences
Aspects | Cyclosporine | Restasis |
|---|---|---|
Form | Oral, IV, topical | Ophthalmic emulsion |
Onset | 1-2 weeks (oral) | 4-6 weeks (eye drops) |
Indications | Broad (transplant, autoimmunity) | Chronic dry eye only |
Dosage | 2.5–5 mg/kg/day (oral) | 1 drop/eye BID |
Does Cyclosporine Cause Weight Gain?
Generally, no.
However, in the long run, it may lead to weight gain.
Yes, you see it clearly: cyclosporine can cause weight gain in some people, although it is not one of its most common side effects.
Why Might Cyclosporine Cause Weight Gain?
The exact mechanisms aren’t fully understood, but several factors may contribute:
Fluid Retention (Edema):
- Cyclosporine can cause the body to retain sodium and water, leading to swelling (especially in the legs, ankles, or around the eyes). This can result in a temporary increase in weight due to fluid retention, not fat accumulation.
Increased Appetite:
- Some individuals report an increase in appetite while taking cyclosporine, which could contribute to weight gain over time.
Metabolic Effects:
- Cyclosporine may affect fat metabolism or insulin sensitivity in some people, potentially leading to changes in body composition or weight.
Reduced Physical Activity:
- Patients on cyclosporine often have chronic conditions (like organ transplants or autoimmune diseases), which may limit physical activity and contribute to weight changes.
How Common Is It?
Weight gain is not among the most frequently reported side effects of cyclosporine, but it has been noted in clinical studies and patient reports. The degree of weight change varies from person to person.
What Should You Do If You’re Gaining Weight?
- Talk to your doctor: They can help determine if the weight gain is due to cyclosporine or another cause (such as fluid retention, diet, or reduced activity).
- Monitor your diet and fluid intake: Reducing salt intake can help minimize fluid retention.
- Stay active: Gentle exercise, as tolerated and approved by your healthcare provider, can help manage weight and overall health.
In summary, cyclosporine can contribute to weight gain, usually due to fluid retention or increased appetite.
It’s not universal, and individual responses vary. Always consult your healthcare provider for personalized advice.
Is Cyclosporine Safe In Pregnancy?
It all depends, but cyclosporine is a relatively safe medication to use during pregnancy, and you should take it with caution when its benefits outweigh the risks.
Though doctors recommend that you avoid all unnecessary medications during pregnancy, this is not an option for many pregnant women whose quality of life is significantly impacted without cyclosporine or for those who must continue immunosuppressive therapy to avoid organ rejection.
What are the side effects of cyclosporine?
Since Cyclosporine is a potent and effective immunosuppressant, it can cause a range of side effects, some of which can be serious.
Common Side Effects of Cyclosporine:
These are side effects that may occur in many people taking the drug:
- Tremors or shaking
- Headache
- Gum overgrowth (gingival hyperplasia)
- Increased hair growth (hirsutism)
- High blood pressure (hypertension)
- Nausea or upset stomach
- Diarrhea
- Loss of appetite
- Fatigue or weakness
Less Common but Serious Side Effects:
These require medical attention and may indicate a need for dose adjustment or discontinuation:
- Kidney problems (the most common profound side effect):
- Symptoms may include changes in urination, swelling in the legs or feet
- High potassium levels (hyperkalemia)
- Increased risk of infections (due to immune suppression)
- Liver problems:
- Symptoms: yellowing of skin/eyes (jaundice), dark urine, abdominal pain
- High blood pressure that is difficult to control
- Neurological effects:
- Tremors, confusion, seizures (rare)
- Increased risk of specific cancers, especially skin cancer (due to long-term immune suppression)
Rare but Potentially Life-Threatening Side Effects:
- Severe allergic reactions (rash, itching/swelling, difficulty breathing)
- Pancreatitis (inflammation of the pancreas)
- Blood disorders (e.g., low white blood cells, anemia)
Drug Interactions and Monitoring:
Cyclosporine interacts with many other medications and can be affected by food, supplements, and herbal products. It requires:
- Regular blood tests to monitor kidney and liver function
- Blood pressure monitoring
- Monitoring of drug levels in the blood (therapeutic drug monitoring)
Important Notes:
- Always take Cyclosporine exactly as prescribed.
- Avoid grapefruit and grapefruit juice, as they can significantly increase drug levels and the risk of toxicity.
- Inform your doctor about all other medications, supplements, or herbal products you are taking.
If you’re taking Cyclosporine and experience new or worsening symptoms—especially those related to your kidneys, liver, blood pressure, or signs of infection—contact your healthcare provider immediately.
Can I Drink Alcohol While Taking Cyclosporine?
No, you can’t, and you shouldn’t either.
Most drugs have drug interactions with alcohol, and cyclosporine is no exception.
To avoid drug interactions, you shouldn’t drink alcohol when you are on any medications.
Does Cyclosporine Cause Hair Growth?
Yes, cyclosporine can cause increased hair growth (a condition known as hirsutism or hypertrichosis) in some individuals, both humans and animals.
Why Does Cyclosporine Cause Hair Growth?
Although the exact mechanism isn’t fully understood, researchers believe cyclosporine affects hair follicles by altering the immune environment and possibly influencing:
- Keratinocyte proliferation (cells that make up the hair shaft and follicle)
- Local growth factors involved in hair growth
- Immune-modulated pathways that affect hair follicle cycling
Cyclosporine is a calcineurin inhibitor that suppresses specific immune responses, potentially prolonging the anagen (growth) phase of the hair cycle and leading to increased hair growth in some individuals.
In Humans:
- Common in transplant patients or those using cyclosporine for autoimmune diseases.
- Hair growth is often generalized but can be more noticeable on the face, arms, or other areas of the body.
- The effect is usually reversible after stopping the medication.
In Dogs:
- Cyclosporine (e.g., Atopica, Optimmune) is commonly used to treat atopic dermatitis and dry eye.
- One well-known side effect in dogs is excessive hair growth, especially around the face, neck, and tail.
- Owners often notice their dog’s coat becoming thicker or darker.
- Like in humans, this effect is typically irreversible after discontinuing the drug.
Is It Dangerous?
- It’s not harmful in most cases—just a cosmetic side effect.
- However, if hair growth is excessive or accompanied by other unusual symptoms, it’s worth discussing with your doctor or veterinarian.
Summary:
| Species | Effect | Notes |
|---|---|---|
| Humans | Increased body or facial hair | Usually reversible after stopping the drug |
| Dogs | Thicker or darker coat | Common with Atopica® or Optimmune® use |
So, yes—cyclosporine can cause hair growth, and while it’s generally harmless, it’s a known side effect to be aware of.
Cyclosporine Precautions and Drug Interactions
Cyclosporine’s metabolism involves the liver enzyme CYP3A4 and the P-glycoprotein (P-gp) transport system.
Many interactions occur by inhibiting or inducing these pathways, leading to dangerously high or low cyclosporine levels.
The table below outlines key drug interactions, followed by essential precautions.
| Interaction Type | Effect of Cyclosporine | Common Examples | Clinical Implication |
|---|---|---|---|
| Drugs that INCREASE levels (CYP3A4/P-gp inhibitors) | Raises blood concentration, increasing toxicity risk (e.g., kidney damage). | Antifungals: Ketoconazole, Fluconazole Antibiotics: Clarithromycin, Erythromycin Others: Diltiazem, Verapamil, Amiodarone | Risk of nephrotoxicity. Requires dose reduction and close monitoring. |
| Drugs that DECREASE levels (CYP3A4/P-gp inducers) | Lowers blood concentration, increasing the risk of rejection or treatment failure. | Anticonvulsants: Phenytoin, Phenobarbital, Carbamazepine Antibiotics: Rifampin | Risk of under-immunosuppression. Requires a dose increase and close monitoring. |
| Additive Nephrotoxicity | Increases the risk of kidney damage through the combined toxic effect. | Aminoglycosides, Amphotericin B, NSAIDs (e.g., ibuprofen, naproxen) | Avoid concurrent use if possible; monitor kidney function meticulously. |
Critical Herbal & Food Interactions
Concurrent use of herbal supplements is common, and cyclosporine has one of the highest numbers of documented herb-drug interactions among immunosuppressants.
St. John’s Wort: Must be avoided. It potently induces CYP3A4 and P-gp, leading to a dramatic drop in cyclosporine levels and risk of organ rejection.
Grapefruit (and Juice): Must be avoided. It inhibits intestinal CYP3A4, significantly increasing cyclosporine absorption and the risk of toxicity.
Other Notable Herbs: Evidence, often from animal studies, suggests caution with:
Increase Levels: Chamomile, berberine, cannabidiol.
Decrease Levels: Ginger, licorice, Scutellariae radix.
Key Precautions and Required Monitoring
Managing cyclosporine involves active vigilance for side effects and regular testing.
Nephrotoxicity (Kidney Damage): This is the most common and serious adverse effect. Kidney function must be checked regularly.
Hypertension (High Blood Pressure): Frequently occurs and requires monitoring and management.
Other Common side effects include tremor, excessive hair growth (hypertrichosis), gum overgrowth (gingival hyperplasia), nausea, diarrhea, and high blood lipids.
Increased Infection & Cancer Risk: As an immunosuppressant, it lowers your body’s defenses against infections and slightly increases the risk of certain cancers (such as lymphoma and skin cancer).
Essential Blood Tests: Therapeutic Drug Monitoring (TDM) is mandatory. Dosing is guided by trough blood levels (e.g., often kept between 50 and 150 ng/mL, depending on the indication). Regular checks of serum creatinine (for kidney function), blood pressure, potassium, magnesium, and liver enzymes are also crucial.
How Does Cyclosporine Work For Dry eyes?
Cyclosporine is commonly used to treat dry eye syndrome (keratoconjunctivitis sicca, also known as KCS) in both humans and animals.
It doesn’t act as a lubricant like artificial tears; instead, it helps stimulate natural tear production by targeting the underlying immune-mediated inflammation that causes or worsens dry eye.
What Causes Dry Eye?
Dry eye occurs when the lacrimal (tear) glands don’t produce enough tears or when the quality of the tears is poor. In many cases—especially in dogs and some humans—it’s caused by immune-mediated inflammation of the lacrimal glands and surrounding tissues.
This inflammation damages the gland cells responsible for tear production, leading to:
- Reduced tear secretion
- Red, irritated eyes
- Corneal damage over time
How Cyclosporine Works for Dry Eye:
Cyclosporine is an immunosuppressant that inhibits T-cell activation, a key part of the immune response that contributes to chronic inflammation.
Step-by-step mechanism:
Blocks Calcineurin Activation:
- Cyclosporine binds to a protein called cyclophilin inside immune cells (especially T-cells).
- This complex inhibits calcineurin, an enzyme necessary for T-cell activation.
Reduces Inflammatory Cytokines:
- By suppressing T-cell activity, cyclosporine reduces the release of inflammatory molecules, such as interleukin-2 (IL-2).
- This helps calm the immune response against the lacrimal glands.
Restores Tear Production:
- With less inflammation, the damaged tear glands can begin to heal.
- Over time, this leads to increased natural tear production and improved eye moisture.
Improves Ocular Surface Health:
- Reduced inflammation also helps protect the cornea and conjunctiva from further damage.
Use in Dogs (and Humans):
- In dogs, cyclosporine ophthalmic ointment (e.g., Optimmune) is a standard and effective treatment for chronic dry eye.
- It’s often used long-term to maintain tear production.
- It typically takes 2–4 weeks of consistent use before improvement is observed, and maximum benefit may take several months.
Benefits of Cyclosporine for Dry Eye:
- Stimulates natural tear production (unlike artificial tears, which only lubricate)
- Reduces inflammation on the ocular surface
- It helps prevent corneal damage and scarring
- It can be used long-term with minimal systemic side effects when applied topically
Considerations:
- It may take several weeks to show improvement
- Not effective for every case of dry eye (especially if the cause is not immune-mediated)
- Some animals may need additional therapies (e.g., artificial tears, other medications)
Where To Buy Cyclosporine Eye Drops For Dogs?
#1. Many branded Cyclosporine Eye Drops for dogs are available online, including Atopica, Neoral, Sandimmune, and Optimmune.
You can order them online, such as from Chewy or PetMeds, or at your local animal pharmacies.
There are certainly cheaper generic alternatives available for your dog; choose the one that best suits you.
#2. If your dogs are allergic to certain ingredients in branded or generic eye drops, consider contacting a compounding pharmacy for customized formulations to avoid potential allergic reactions.
#3. If your compounding pharmacies are short of cyclosporine raw materials, you must import small quantities to compound.
The cost for 100 grams is around 350~550 USD, which the pharmacists can compound into thousands of bottles of eye drops for dogs.
How Long Can A Dog Take Cyclosporine?
The length of time a dog can safely take cyclosporine depends on several factors, including:
- The reason for use (e.g., atopic dermatitis, immune-mediated conditions, organ transplants)
- The dog’s overall health, especially kidney and liver function
- The formulation and dosage of cyclosporine (e.g., oral capsule or liquid)
- Veterinary supervision and monitoring
Short-Term Use (Weeks to Months):
- Many dogs start with cyclosporine for acute flare-ups of allergies or skin issues.
- It can be used safely for weeks to a few months under veterinary supervision.
Long-Term Use (Months to Years):
- For chronic conditions like atopic dermatitis, dogs may stay on cyclosporine long-term, sometimes for years, especially if other treatments (like steroids or antihistamines) are ineffective or cause intolerable side effects.
- However, long-term use requires regular veterinary monitoring to check for potential side effects.
Potential Side Effects & Monitoring Needs:
Cyclosporine can cause side effects in dogs, especially with prolonged use. These may include:
- GI upset (vomiting, diarrhea)
- Gingival hyperplasia (gum overgrowth)
- Increased appetite or weight gain
- Kidney or liver dysfunction (especially with high doses or long-term use)
- Higher susceptibility to infections
Because of these risks, vets typically:
- Perform baseline bloodwork before starting treatment
- Recommend periodic blood tests (every 6–12 months or more frequently if needed)
- Monitor for changes in appetite, weight, energy level, or urination
Veterinary Guidance Is Essential:
Your veterinarian will determine how long your dog should stay on cyclosporine based on:
- How well the condition is controlled
- Any side effects your dog experiences
- Results of blood tests and physical exams
They may also try to adjust the dose or switch medications over time, if possible.
How Does Cyclosporine Work For Psoriasis?
Psoriasis is a chronic autoimmune skin condition in which the immune system mistakenly attacks healthy skin cells.
It causes:
- Rapid turnover of skin cells
- Inflammation
- Thick, red, scaly patches (plaques)
The immune system plays a central role, particularly certain types of white blood cells called T-cells, which become overactive and trigger inflammation in the skin.
How Cyclosporine Works For Psoriasis:
Step-by-step Mechanism:
Blocks Calcineurin Activity:
- Cyclosporine binds to a protein in T-cells called cyclophilin.
- This complex inhibits calcineurin, an enzyme that typically activates T cells.
Suppresses T-cell Activation:
- When calcineurin is blocked, T-cells don’t become fully activated.
- This reduces the release of pro-inflammatory cytokines, such as IL-2, which generally promote inflammation and skin cell overgrowth.
Reduces Inflammation and Slows Skin Cell Growth:
- With fewer active T cells and reduced inflammation, the rapid skin cell turnover characteristic of psoriasis slows.
- This leads to improvements in redness, scaling, and plaque thickness.
Clinical Effect:
- Cyclosporine can lead to a rapid improvement in psoriasis symptoms (often within weeks).
- It is beneficial for severe psoriasis, including:
- Plaque psoriasis
- Pustular psoriasis
- Erythrodermic psoriasis
However, it is generally used for short-term control due to potential side effects (especially on the kidneys and immune system).
Important Considerations:
- Not a cure: Symptoms often return after stopping the drug.
- Requires monitoring: Regular blood tests are necessary to monitor kidney function and drug levels.
- Not first-line: Usually reserved for moderate-to-severe cases that are unresponsive to topical treatments or phototherapy.
Disclaimer:
This content is for informational purposes only and is intended for business-to-business communication within the pharmaceutical industry. It is not intended as medical advice. The manufacture, import, and use of API must comply with all applicable laws and regulations in the relevant country or region.
This blog post is informational only and does not constitute medical advice.
Always consult a healthcare professional before starting any new medication or treatment.
