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Temsirolimus | CAS No: 162635-04-3 | GMP-certified suppliers
A medication that treats renal cell carcinoma by inhibiting mTOR, with potential applications in oncology and immunosuppressive therapies, requiring strict quality control for pharmaceutical sourcing.
Therapeutic categories
Primary indications
- For the treatment of renal cell carcinoma (RCC)
- Also investigated for use/treatment in breast cancer, lymphoma (unspecified), rheumatoid arthritis, and multiple myeloma
Product Snapshot
- Temsirolimus is formulated as an injectable solution and concentrate for intravenous administration
- It is primarily indicated for the treatment of renal cell carcinoma and has been investigated for use in breast cancer, lymphoma, rheumatoid arthritis, and multiple myeloma
- The product is approved and marketed in key regulatory regions including the US, Canada, and the European Union
Clinical Overview
Temsirolimus functions as an inhibitor of the mammalian target of rapamycin (mTOR), a serine-threonine kinase involved in regulating cell growth, proliferation, and angiogenesis. The drug binds intracellularly to the immunophilin FKBP-12 to form a complex that specifically inhibits mTOR activity. This inhibition leads to cell cycle arrest in the G1 phase by preventing the phosphorylation of downstream effectors such as p70 S6 kinase and S6 ribosomal protein within the PI3 kinase/AKT signaling pathway. In renal cell carcinoma cell lines, temsirolimus decreases the expression of hypoxia-inducible factors HIF-1α and HIF-2α and reduces vascular endothelial growth factor (VEGF), contributing to its antineoplastic effects.
Pharmacokinetic data indicate that temsirolimus acts as both a substrate and an inhibitor of multiple cytochrome P450 enzymes, particularly CYP3A4, as well as a substrate and inhibitor of P-glycoprotein. These interactions necessitate consideration of potential drug-drug interactions during clinical use. Temsirolimus has a narrow therapeutic index and is classified among myelosuppressive and immunosuppressive agents, with adverse effects potentially including hyperglycemia, angioedema, and other toxicities related to immune modulation.
Although temsirolimus has been investigated for other indications, including breast cancer, lymphoma, rheumatoid arthritis, and multiple myeloma, its clinical approval remains focused on RCC treatment.
For pharmaceutical formulation and sourcing, temsirolimus must meet stringent quality specifications, given its complex macrolide lactam structure and narrow therapeutic window. Verification of purity, polymorphic form, residual solvents, and stability profiles is essential. Suppliers should provide comprehensive certificates of analysis and comply with Good Manufacturing Practice (GMP) standards to ensure consistent API quality for clinical and commercial use.
Identification & chemistry
| Generic name | Temsirolimus |
|---|---|
| Molecule type | Small molecule |
| CAS | 162635-04-3 |
| UNII | 624KN6GM2T |
| DrugBank ID | DB06287 |
Pharmacology
| Summary | Temsirolimus is an mTOR inhibitor that forms a complex with FKBP-12 to suppress mTOR kinase activity, leading to cell cycle arrest at the G1 phase. By inhibiting mTOR, temsirolimus blocks phosphorylation of downstream effectors p70S6K and S6 ribosomal protein, disrupting the PI3K/AKT signaling pathway. This results in reduced expression of hypoxia-inducible factors and vascular endothelial growth factor, affecting tumor cell proliferation and angiogenesis, primarily used in renal cell carcinoma. |
|---|---|
| Mechanism of action | Temsirolimus is an inhibitor of mTOR (mammalian target of rapamycin). Temsirolimus binds to an intracellular protein (FKBP-12), and the protein-drug complex inhibits the activity of mTOR that controls cell division. Inhibition of mTOR activity resulted in a G1 growth arrest in treated tumor cells. When mTOR was inhibited, its ability to phosphorylate p70S6k and S6 ribosomal protein, which are downstream of mTOR in the PI3 kinase/AKT pathway was blocked. In in vitro studies using renal cell carcinoma cell lines, temsirolimus inhibited the activity of mTOR and resulted in reduced levels of the hypoxia-inducible factors HIF-1 and HIF-2 alpha, and the vascular endothelial growth factor. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Serine/threonine-protein kinase mTOR | Humans | inhibitor |
ADME / PK
| Absorption | Infused intravenous over 30 - 60 minutes. C<sub>max</sub> is typically observed at the end of infusion |
|---|---|
| Half-life | Temsirolimus exhibits a bi-exponential decline in whole blood concentrations and the mean half-lives of temsirolimus and sirolimus were 17.3 hr and 54.6 hr, respectively. |
| Protein binding | 87% bound to plasma proteins <i>in vitro</i> at a concentration of 100 ng/ml |
| Metabolism | Primarily metabolized by cytochrome P450 3A4 in the human liver. Sirolimus, an equally potent metabolite, is the primary metabolite in humans following IV infusion. Other metabolic pathways observed in <i>in vitro</i> temsirolimus metabolism studies include hydroxylation, reduction and demethylation. |
| Route of elimination | Excreted predominantly in feces (76%), 4.6% of drug and metabolites recovered in urine. 17% of drug was not recovered by either route following a 14-day sample collection. |
| Volume of distribution | 172 L in whole blood of cancer patients; both temsirolimus and sirolimus are extensive distributed partitioned into formed blood elements |
| Clearance | 16.2 L/h (22%) |
Formulation & handling
- Temsirolimus is a small molecule macrolide lactam administered exclusively via intravenous injection or parenteral routes.
- The compound exhibits low water solubility and high lipophilicity (LogP 7.13), requiring appropriate formulation strategies for injection.
- Avoid concomitant use of grapefruit and St. John's Wort due to CYP3A4-mediated drug interaction risks affecting serum levels.
Regulatory status
| Lifecycle | The API is at varying stages of patent protection across key markets, with patents expired or expiring in Canada and the US between 2019 and early 2024, and extended patent protection in the US until 2032. Market maturity differs accordingly, with more opportunities for generic entry in Canada and earlier-expiring US patents, while ongoing exclusivity may limit competition in the US until patent expiry. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Temsirolimus includes multiple packagers serving the Canadian, US, and EU markets, reflecting a broad global presence of branded products. Key patents in the United States extend protection until as late as 2032, with some expiring between 2019 and 2024, indicating both existing and potential generic competition in these regions. Originator companies have established multiple formulations under various brand names across these markets. |
|---|
Safety
| Toxicity | Temsirolimus has been administered to patients with cancer in phase 1 and 2 trials with repeated intravenous doses as high as 220 mg/m2. The risk of several serious adverse events, including thrombosis, bowel perforation, interstitial lung disease (ILD), seizure, and psychosis, is increased with doses of temsirolimus greater than 25 mg. |
|---|
- Temsirolimus exposure above 25 mg is associated with increased risk of thrombosis, bowel perforation, interstitial lung disease, seizure, and psychosis
- Repeated intravenous dosing up to 220 mg/m2 has been evaluated in clinical trials, indicating a narrow safety margin
- Handling should consider potential pulmonary and neurological toxicity inherent to the compound
Temsirolimus is a type of Antineoplastics
Antineoplastics are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) primarily used in the treatment of cancer. These powerful substances inhibit or destroy the growth of cancer cells, thus impeding the progression of malignancies.
Antineoplastics exert their therapeutic effects through various mechanisms. Some APIs interfere with DNA replication, inhibiting the division and proliferation of cancer cells. Others target specific proteins or enzymes involved in tumor growth, effectively blocking their function. Additionally, certain antineoplastic agents induce programmed cell death, known as apoptosis, in cancer cells.
These APIs find application in a wide range of cancer treatments, including chemotherapy, targeted therapy, immunotherapy, and hormone therapy. They are often administered in combination with other drugs to optimize therapeutic outcomes and minimize drug resistance.
Antineoplastics are typically synthesized through complex chemical processes, ensuring high purity and potency. Stringent quality control measures are implemented throughout manufacturing to meet regulatory standards and ensure patient safety.
Although antineoplastics offer significant benefits in treating cancer, they can also cause adverse effects due to their cytotoxic nature. Common side effects include bone marrow suppression, gastrointestinal disturbances, hair loss, and immune system suppression. Close monitoring and supportive care are essential to manage these side effects effectively.
In conclusion, antineoplastics are a vital category of pharmaceutical APIs used in the treatment of cancer. Through their diverse mechanisms of action, these compounds play a critical role in combating malignancies and improving patient outcomes.
Temsirolimus API manufacturers & distributors
Compare qualified Temsirolimus API suppliers worldwide. We currently have 6 companies offering Temsirolimus API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Biocon | Producer | India | India | CoA, GMP, USDMF, WC | 36 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| Laurus Labs | Producer | India | India | CoA, GMP, WC | 50 products |
| Pharmacia & Upjohn | Producer | United States | Ireland | CoA, GMP | 30 products |
| Sandoz | Producer | Austria | Unknown | CoA, USDMF | 58 products |
| Sun Pharma | Producer | India | India | CoA, USDMF | 219 products |
When sending a request, specify which Temsirolimus 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 Temsirolimus 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.
