Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Everolimus API Manufacturers & Suppliers
12 verified results
Commercial-scale Suppliers
Employees: 25+
All certificates
Employees: 260+
All certificates
Employees: 50+
All certificates
Employees: 200+
All certificates
All certificates
All certificates
All certificates
Employees: 10000
All certificates
All certificates
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Everolimus | CAS No: 159351-69-6 | GMP-certified suppliers
A medication that treats advanced hormone receptor‑positive breast cancer, pancreatic neuroendocrine tumors, renal cell carcinoma, and tuberous sclerosis–related lesions to support broad oncology and rare‑disease care.
Therapeutic categories
Primary indications
- Everolimus is indicated for the treatment of postmenopausal women with advanced hormone receptor-positive, HER2-negative breast cancer (advanced HR+ BC) in combination with exemestane, after failure of treatment with letrozole or anastrozole
- Indicated for the treatment of adult patients with progressive neuroendocrine tumors of pancreatic origin (PNET) with unresectable, locally advanced or metastatic disease
- Indicated for the treatment of adult patients with advanced renal cell carcinoma (RCC) after failure of treatment with sunitinib or sorafenib
- Indicated for the treatment of adult patients with renal angiomyolipoma and tuberous sclerosis complex (TSC), not requiring immediate surgery
Product Snapshot
- Everolimus is an oral small‑molecule API supplied mainly as standard tablets, orally disintegrating tablets, and tablets for suspension
- It is used across oncology and rare‑disease portfolios, including HR+ breast cancer, PNET, RCC, renal angiomyolipoma associated with TSC, and SEGA in TSC
- It is approved in the US, Canada, and the EU
Clinical Overview
Everolimus exerts its pharmacological activity by forming a high‑affinity complex with FKBP‑12, which inhibits mTOR activity within the mTORC1 complex while sparing mTORC2. mTORC1 inhibition suppresses downstream signaling pathways that regulate protein synthesis and cell-cycle progression, particularly the transition from G1 to S phase. This leads to reduced cellular proliferation, induction of cell cycle arrest, and promotion of apoptosis. Inhibition of hypoxia-inducible factor expression contributes to reduced vascular endothelial growth factor production, thereby limiting angiogenesis and glucose utilization in target tissues.
Absorption, distribution, metabolism, and excretion characteristics are strongly influenced by cytochrome P450 3A and by P‑glycoprotein transport. Everolimus is both a substrate and inhibitor of CYP3A4 and P‑gp, resulting in high susceptibility to drug–drug interactions and variability in systemic exposure. The therapeutic window is narrow, necessitating careful dose adjustment. Reported safety concerns include stomatitis, cytopenias, hyperlipidemia, hyperglycemia, increased infection risk, impaired wound healing, and noninfectious pneumonitis. Toxicity risk increases in the presence of metabolic inhibitors or reduced hepatic clearance.
Everolimus is widely used across oncology and transplant-related contexts under various regional brands. For API procurement, manufacturers should emphasize control of polymorphic form, impurity profiles consistent with ICH guidelines, and validated processes for ensuring consistent potency and stability due to the molecule’s sensitivity to oxidative and hydrolytic degradation.
Identification & chemistry
| Generic name | Everolimus |
|---|---|
| Molecule type | Small molecule |
| CAS | 159351-69-6 |
| UNII | 9HW64Q8G6G |
| DrugBank ID | DB01590 |
Pharmacology
| Summary | Everolimus forms a complex with FKBP‑12 to inhibit mTOR, suppressing downstream signaling pathways that regulate cell‑cycle progression, protein synthesis, and cellular metabolism. This blockade reduces proliferation, angiogenesis, and glucose uptake while promoting growth arrest and apoptosis in susceptible cells. Its therapeutic intent centers on conditions driven by dysregulated mTOR activity, including certain solid tumors and tuberous sclerosis complex–associated lesions. |
|---|---|
| Mechanism of action | Everolimus is a mTOR inhibitor that binds with high affinity to the FK506 binding protein-12 (FKBP-12), thereby forming a drug complex that inhibits the activation of mTOR. This inhibition reduces the activity of effectors downstream, which leads to a blockage in the progression of cells from G1 into S phase, and subsequently inducing cell growth arrest and apoptosis. Everolimus also inhibits the expression of hypoxia-inducible factor, leading to a decrease in the expression of vascular endothelial growth factor. The result of everolimus inhibition of mTOR is a reduction in cell proliferation, angiogenesis, and glucose uptake. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Serine/threonine-protein kinase mTOR | Humans | inhibitor |
ADME / PK
| Absorption | In patients with advanced solid tumors, peak everolimus concentrations are reached 1 to 2 hours after administration of oral doses ranging from 5 mg to 70 mg. Following single doses, Cmax is dose-proportional between 5 mg and 10 mg. At doses of 20 mg and higher, the increase in Cmax is less than dose-proportional, however AUC shows dose-proportionality over the 5 mg to 70 mg dose range. Steady-state was achieved within 2 weeks following once-daily dosing. Dose Proportionality in Patients with SEGA (subependymal giant-cell astrocytomas) and TSC (tuberous sclerosis complex): In patients with SEGA and TSC, everolimus Cmin was approximately dose-proportional within the dose range from 1.35 mg/m2 to 14.4 mg/m2. |
|---|---|
| Half-life | ~30 hours. |
| Protein binding | ~ 74% in both healthy patients and those with moderate hepatic impairment. |
| Metabolism | Everolimus is a substrate of CYP3A4 and PgP (phosphoglycolate phosphatase). Three monohydroxylated metabolites, two hydrolytic ring-opened products, and a phosphatidylcholine conjugate of everolimus were the 6 primary metabolites detected in human blood. In vitro, everolimus competitively inhibited the metabolism of CYP3A4 and was a mixed inhibitor of the CYP2D6 substrate dextromethorphan. |
| Route of elimination | After a single dose of radiolabeled everolimus was given to transplant patients receiving cyclosporine, the majority (80%) of radioactivity was recovered from the feces and only a minor amount (5%) was excreted in urine. |
| Volume of distribution | The blood-to-plasma ratio of everolimus is 17% to 73%. |
| Clearance | Following a 3 mg radiolabeled dose of everolimus, 80% of the radioactivity was recovered from the feces, while 5% was excreted in the urine. |
Formulation & handling
- Low aqueous solubility and high lipophilicity require solubilization‑enhancing strategies for oral tablets, including solid dispersion or lipid‑based approaches.
- As an orally administered small‑molecule macrolide lactam, absorption is food‑sensitive, so formulations should support consistent intake relative to meals.
- Handling should account for CYP3A4/PGP interaction potential, with packaging and labeling emphasizing avoidance of grapefruit products and St. John’s wort.
Regulatory status
| Lifecycle | The API shows a mature market profile in Canada and partial maturity in the US, with several key patents already expired and the final U.S. protection extending to 2026. Across the US, Canada, and the EU, market conditions suggest progressing generic availability as remaining exclusivities lapse. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Everolimus is supplied by a small group of firms, with the originator responsible for the branded product and additional companies involved mainly in packaging and distribution. The brand is marketed across the US, Canada, and the EU, indicating broad global penetration. Multiple key patents have already expired, with one US patent extending to 2026, suggesting that generic competition is present in some regions and may further expand as remaining protections lapse. |
|---|
Safety
| Toxicity | IC50 of 0.63 nM. |
|---|
- Potent mTOR inhibition (IC50 ~0
- 63 nM) warrants controlled handling to limit inadvertent exposure
- Avoid aerosolization or dust generation during processing
Everolimus is a type of Immunosuppressants
Immunosuppressants are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in medical treatments. These substances are designed to suppress or weaken the immune system's response, making them invaluable in various therapeutic applications.
Immunosuppressants find extensive use in the management of autoimmune diseases, organ transplantation, and the prevention of rejection reactions. By modulating the immune system's activity, these APIs help control excessive immune responses that can lead to tissue damage and chronic inflammation.
There are different classes of immunosuppressants, including corticosteroids, calcineurin inhibitors, antimetabolites, and biologics. Each class targets specific immune pathways to achieve the desired therapeutic effect. Corticosteroids, for instance, are known for their potent anti-inflammatory properties, making them effective in managing conditions such as rheumatoid arthritis and asthma.
Calcineurin inhibitors like cyclosporine and tacrolimus act by inhibiting the activity of calcineurin, a protein involved in immune cell activation. These drugs are commonly used in organ transplantation to prevent the immune system from attacking the transplanted organ.
Antimetabolites interfere with DNA synthesis and cell proliferation, thereby dampening immune responses. They are often prescribed for conditions like psoriasis and rheumatoid arthritis.
Biologic immunosuppressants, such as monoclonal antibodies, target specific immune cells or molecules involved in the disease process. They have revolutionized the treatment of autoimmune diseases like rheumatoid arthritis, Crohn's disease, and psoriasis.
Immunosuppressants require careful administration and monitoring due to their potential side effects and interactions with other medications. Close collaboration between healthcare professionals, pharmacists, and patients is essential to ensure the safe and effective use of these APIs in various therapeutic settings.
Overall, immunosuppressants represent a critical category of pharmaceutical APIs that significantly contribute to improving patients' quality of life by controlling the immune system's activity and managing various autoimmune conditions and transplantation outcomes.
Everolimus (Immunosuppressants), classified under Immunomodulators
Immunomodulators, a category of pharmaceutical active pharmaceutical ingredients (APIs), are substances that help regulate and modify the immune response of an individual. These compounds play a crucial role in treating various immune-related disorders and diseases. Immunomodulators work by either enhancing or suppressing the immune system, depending on the specific condition being treated.
Immunomodulators are used in the treatment of autoimmune disorders, such as rheumatoid arthritis, multiple sclerosis, and psoriasis. By suppressing the immune system, these APIs help reduce the overactive immune response associated with these conditions, thereby alleviating symptoms and preventing further damage to the body's tissues.
On the other hand, immunomodulators are also employed to boost the immune system in cases of immunodeficiency disorders. These APIs stimulate the immune response, enabling the body to better fight off infections and diseases. Additionally, immunomodulators are utilized in the prevention and treatment of organ transplant rejection, where they help modulate the immune system to accept the transplanted organ.
The development and production of immunomodulators require rigorous testing and quality control to ensure their safety and efficacy. Pharmaceutical companies carefully formulate these APIs into various dosage forms, including tablets, capsules, injections, and topical preparations, to cater to different patient needs.
In summary, immunomodulators form a vital category of pharmaceutical APIs that regulate and modify the immune system. With their ability to modulate immune responses, these compounds contribute significantly to the management and treatment of various immune-related disorders and diseases, improving the quality of life for many patients.
Everolimus API manufacturers & distributors
Compare qualified Everolimus API suppliers worldwide. We currently have 12 companies offering Everolimus API, with manufacturing taking place in 6 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Adley Formulations | Producer | India | India | CoA, GMP | 14 products |
| Aurora Industry Co., Ltd | Distributor | China | China | BSE/TSE, CEP, CoA, GMP, ISO9001, MSDS, USDMF | 250 products |
| Biocon | Producer | India | India | CoA, GMP, USDMF, WC | 36 products |
| BrightGene | Producer | China | China | CoA, USDMF | 11 products |
| CCSB-Chunghwa Chemical Sy... | Producer | Taiwan | Taiwan | BSE/TSE, CEP, CoA, EDMF/ASMF, FDA, GMP, MSDS, USDMF | 27 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| Lek Pharma | Producer | Slovenia | Slovenia | CoA, GMP | 32 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Natco Pharma | Producer | India | India | CoA, USDMF, WC | 40 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, ISO9001 | 157 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Yacht Bio-Tech | Producer | China | China | CoA, USDMF | 2 products |
When sending a request, specify which Everolimus API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Everolimus API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Everolimus API
Sourcing
What matters most when sourcing GMP-grade Everolimus?
Which documents are typically required when sourcing Everolimus API?
Which manufacturers are known to produce Everolimus API?
How can I request quotes for Everolimus API from GMP suppliers?
Is a GMP audit report available for Everolimus manufacturers?
How many suppliers offer Everolimus API on Pharmaoffer?
Which countries are known to manufacture Everolimus API?
Which certifications do suppliers of Everolimus usually hold?
Technical
What is Everolimus (CAS 159351-69-6) used for?
Which therapeutic class does Everolimus fall into?
What conditions is Everolimus mainly prescribed for?
How does Everolimus work?
What should someone know about the safety or toxicity profile of Everolimus?
What are important formulation and handling considerations for Everolimus as an API?
Is Everolimus a small molecule?
Are there special stability concerns for oral Everolimus?
Regulatory
Where is Everolimus approved or in use globally?
What’s the regulatory and patent landscape for Everolimus right now?
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Everolimus procurement?
Is Everolimus included in the PRO Data Insights coverage?
Where can I access the API market report for Everolimus?
