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PubChem
Name: Sirolimus
PubChem Compound ID: 313006
Description: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
Molecular formula: C51H79NO13
Molecular weight: 914.172 g/mol
Synonyms:
NCI60_001851
DrugBank
Identification
Name: Sirolimus
Name (isomeric): DB00877
Drug Type: small molecule
Description: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.
Synonyms:
Antibiotic AY 22989; rapamycin
Brand: Rapamune, Rapamycin
Category: Anti-Bacterial Agents, Antifungal Agents, Antifungals, Macrolides, Antibiotics, Antineoplastic, Immunosuppressive Agents
CAS number: 53123-88-9
Pharmacology
Indication: For the prophylaxis of organ rejection in patients receiving renal transplants.
Pharmacology: Sirolimus, a macrocyclic lactone produced by Streptomyces hygroscopicus, is an immunosuppressive agent indicated for the prophylaxis of organ rejection in patients receiving renal transplants. It is recommended that sirolimus be used in a regimen with cyclosporine and corticosteroids.
Mechanism of Action:
Sirolimus inhibits T lymphocyte activation and proliferation that occurs in response to antigenic and cytokine (Interleukin IL-2, IL-4, and IL-15) stimulation by a mechanism that is distinct from that of other immunosuppressants. Sirolimus also inhibits antibody production. In cells, sirolimus binds to the immunophilin, FK Binding Protein-12 (FKBP-...
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Protein binding: 92%
Half Life: 57-63 hours
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
ItraconazoleItraconazole may increase the effect and toxicity of sirolimus.
TrastuzumabTrastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
TrandolaprilIncreased risk of angioedema. Monitor for signs and symptoms of facial and systemic edema and/or erythema.
ErythromycinThe macrolide, erythromycin, may increase the serum concentration of sirolimus.
ClarithromycinThe macrolide, clarithromycin, may increase the serum concentration of sirolimus.
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