Temsirolimus

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Temsirolimus is an ofp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2007. Its mechanism of action is classified as mTOR Inhibitors and Protein Kinase Inhibitors. DrugCentral lists 4 molecular targets, including MTOR, ABCB1 and FKBP1A. Recorded indications include Mantle cell lymphoma and Renal cell carcinoma.

• Approval status: ofp (first approved 2007 by the FDA).
• Drug class: Kinase Inhibitor; mTOR Inhibitor Immunosuppressant.
• Mechanism of action: mTOR Inhibitors; Protein Kinase Inhibitors.
• Molecular targets: MTOR, ABCB1, FKBP1A and FKBP3 (4 listed in DrugCentral).
• Indications: Mantle cell lymphoma and Renal cell carcinoma.
• ATC code: L01EG01 (Mammalian target of rapamycin (mTOR) kinase inhibitors).
• Molecular formula: C56H87NO16; molecular weight 1030.30 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Mantle cell lymphoma
• Renal cell carcinoma

Contraindications (17)

• Acute infectious disease
• Breastfeeding (mother)
• Cerebrovascular accident
• Diabetes mellitus
• Disease of liver
• Gastrointestinal perforation
• Hyperbilirubinemia
• Hyperglycemia
• Hyperlipidemia
• Impaired wound healing
• Interstitial pneumonia
• Kidney disease
• Malignant neoplasm of brain
• Perioperative care
• Pregnancy, function
• Secondary malignant neoplasm of cerebrum
• Surgical procedure

Mechanism & targets

• Mechanism of action (MoA): mTOR Inhibitors; Protein Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor; mTOR Inhibitor Immunosuppressant

Molecular targets (4)

Target	Gene	Action	Activity
Serine/threonine-protein kinase mTOR	MTOR	unknown	IC50 5.75
Multidrug resistance protein 1	ABCB1	unknown	—
Peptidyl-prolyl cis-trans isomerase FKBP1A	FKBP1A	inhibitor	—
Peptidyl-prolyl cis-trans isomerase FKBP3	FKBP3	unknown	—

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2007-11-19	EMA	—	Pfizer Limited	Yes
2007-05-30	FDA	—	PF PRISM CV

ATC classification

ATC code	Therapeutic hierarchy
L01EG01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Mammalian target of rapamycin (mTOR) kinase inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Disease progression	772.8
Pneumonitis	178.3
Dehydration	152.3
Mucosal inflammation	149.7
Neoplasm progression	142.3
Hypertriglyceridaemia	138.6
Pleural effusion	133.3
Stomatitis	129.8
Interstitial lung disease	127.3
Thrombocytopenia	118.8
Hyperglycaemia	116.3
Death	97.2

Chemical structure

• Molecular formula: C₅₆H₈₇NO₁₆
• Molecular weight: 1030.30 g/mol
• CAS number: 162635-04-3
• InChIKey: CBPNZQVSJQDFBE-FUXHJELOSA-N
• PubChem CID: 5284616

CO[C@@H]1C[C@H](C[C@@H](C)[C@@H]2CC(=O)[C@H](C)\C=C(C)\[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)\C=C\C=C\C=C(C)\[C@H](C[C@@H]3CC[C@@H](C)[C@@](O)(O3)C(=O)C(=O)N3CCCC[C@H]3C(=O)O2)OC)CC[C@H]1OC(=O)C(C)(CO)CO

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Temsirolimus used for?

DrugCentral lists the following indications for Temsirolimus: Mantle cell lymphoma and Renal cell carcinoma.

How does Temsirolimus work?

Temsirolimus is classified as mTOR Inhibitors and Protein Kinase Inhibitors; its molecular targets in DrugCentral include MTOR, ABCB1, FKBP1A (inhibitor) and FKBP3.

When was Temsirolimus first approved?

Temsirolimus was first approved by the FDA in 2007.

What drug class does Temsirolimus belong to?

Temsirolimus is in the Kinase Inhibitor class.

What is the chemical formula of Temsirolimus?

Temsirolimus has the molecular formula C56H87NO16 and a molecular weight of 1030.30 g/mol.

Sources

• DrugCentral drug card 4161 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201182 — compound record and bioactivity
• PubChem CID 5284616 — chemical identifiers
• DrugBank DB00877 — drug record
• FDA UNII 624KN6GM2T — substance identity
• DailyMed: FDA labels for Temsirolimus — current prescribing information (label search)
• UniProt P42345 (MTOR) — target protein
• UniProt P08183 (ABCB1) — target protein
• UniProt P62942 (FKBP1A) — target protein
• UniProt Q00688 (FKBP3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.