Thiotepa

Alkylating Drug — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Thiotepa is an ofp drug in the Alkylating Drug class catalogued in DrugCentral. It was first approved by the FDA in 1959. Its mechanism of action is classified as Alkylating Activity. DrugCentral lists 1 molecular target, including CYP2B6. Recorded indications include Allogeneic bone marrow transplantation, Carcinoma of female breast, Hodgkin's disease and Malignant lymphoma.

• Approval status: ofp (first approved 1959 by the FDA).
• Drug class: Alkylating Drug.
• Mechanism of action: Alkylating Activity.
• Molecular targets: CYP2B6 (1 listed in DrugCentral).
• Indications: Allogeneic bone marrow transplantation, Carcinoma of female breast, Hodgkin's disease, Malignant lymphoma and Malignant tumor of ovary and others.
• ATC code: L01AC01 (Ethylene imines).
• Molecular formula: C6H12N3PS; molecular weight 189.22 g/mol.

Indications & contraindications

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

Indications (10)

• Allogeneic bone marrow transplantation
• Carcinoma of female breast
• Hodgkin's disease
• Malignant lymphoma
• Malignant tumor of ovary
• Malignant tumor of urinary bladder
• Non-Hodgkin's lymphoma
• Pericardial Malignant Effusions
• Peritoneal Malignant Effusions
• Pleural Malignant Effusions

Contraindications (10)

• Acute infectious disease
• Anemia
• Blood coagulation disorder
• Bone marrow depression
• Breastfeeding (mother)
• Disease of liver
• Kidney disease
• Leukopenia
• Pregnancy, function
• Thrombocytopenic disorder

Mechanism & targets

• Mechanism of action (MoA): Alkylating Activity
• Established pharmacologic class: Alkylating Drug

Molecular targets (1)

Target	Gene	Action	Activity
Cytochrome P450 2B6	CYP2B6	inhibitor	Ki 5.32

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2021-03-26	EMA	—	RIEMSER Pharma GmbH
2019-03-26	PMDA	—	Sumitomo Dainippon Pharma
1959-03-09	FDA	—	—	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01AC01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ALKYLATING AGENTS › Ethylene imines

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
Acute graft versus host disease in skin	1770.3
Mucosal inflammation	1745.4
Acute graft versus host disease	1597.6
Cytomegalovirus infection reactivation	1372.3
Cytomegalovirus infection	1296.8
Venoocclusive liver disease	1258.7
Human herpesvirus 6 infection	1173.0
Adenovirus infection	1080.8
Acute graft versus host disease in intestine	1005.8
Febrile neutropenia	1005.5
Graft versus host disease	899.7
Chronic graft versus host disease	879.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Thiotepa is on its molecule page.

• Molecular formula: C₆H₁₂N₃PS
• Molecular weight: 189.22 g/mol
• CAS number: —
• InChIKey: FOCVUCIESVLUNU-UHFFFAOYSA-N
• PubChem CID: 5453

S=P(N1CC1)(N1CC1)N1CC1

Frequently asked questions

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

What is Thiotepa used for?

DrugCentral lists the following indications for Thiotepa: Allogeneic bone marrow transplantation, Carcinoma of female breast, Hodgkin's disease, Malignant lymphoma, Malignant tumor of ovary, Malignant tumor of urinary bladder, Non-Hodgkin's lymphoma and Pericardial Malignant Effusions and others.

How does Thiotepa work?

Thiotepa is classified as Alkylating Activity; its molecular targets in DrugCentral include CYP2B6 (inhibitor).

When was Thiotepa first approved?

Thiotepa was first approved by the FDA in 1959.

What drug class does Thiotepa belong to?

Thiotepa is in the Alkylating Drug class.

What is the chemical formula of Thiotepa?

Thiotepa has the molecular formula C6H12N3PS and a molecular weight of 189.22 g/mol.

Sources

• DrugCentral drug card 2638 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL671 — compound record and bioactivity
• PubChem CID 5453 — chemical identifiers
• DrugBank DB04572 — drug record
• FDA UNII 905Z5W3GKH — substance identity
• DailyMed: FDA labels for Thiotepa — current prescribing information (label search)
• UniProt P20813 (CYP2B6) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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