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Thiotepa

Alkylating Agent · Anticancer Drugs

Also known as Thio-TEPA, triethylenethiophosphoramide

Alkylating AgentAnticancer Drugs
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • AdalimumabSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter
  • BusulfanSevereDatabaseDDInter
  • CarboplatinSevereDatabaseDDInter

Mechanism

Thiotepa is an ethylenimine derivative that does not require an active intermediate to exert its effects. It forms stable ethyleneimine derivatives which have antitumor activity by damaging DNA and causing cross-links. This mechanism results in the inhibition of nucleic acid synthesis.

Indications

Conditioning treatment before haematopoietic stem cell transplantation in the treatment of haematological disease or solid tumours, in combination with other chemotherapyovarian cancerbladder cancerhigh-dose chemotherapy regimens (primarily)

Dosing

Adult
0.3–0.4 mg/kg i.v. at 1–4 week intervals (consult local protocol)

Pharmacokinetics

Onset
not specified
Peak effect
not specified
Protein binding
not specified
Metabolism
Metabolized by CYP2B6 and hepatic microsomes (N-demethylation)

Contraindications

  • Acute porphyrias

Side effects

Common
Alopeciaamenorrhoeaanaemiaanxietyappetite decreasedarrhythmiasarthralgiaastheniaazoospermiacataractchillscognitive disorderconfusionconjunctivitisconstipationcoughcystitisdeliriumdiarrhoeadizzinessdysuriaembolismencephalopathyextrapyramidal symptomsfevergastrointestinal discomfortgastrointestinal disordersgeneralised oedemagraft versus host diseasehaemorrhageheadachehearing impairmentheart failurehepatic disordershyperglycaemiahypersensitivityhypertensionhypopituitarismincreased risk of infectioninfertilityintracranial aneurysmintracranial haemorrhageleucopenialymphoedemamenopausal symptomsmucositismulti organ failuremyalgianauseamyelosuppressionmucosal toxicitycentral nervous system toxicitymucositis (to a lesser extent)leukopenic nadirs at 2 weeksplatelet nadirs at 3 weeks
Serious
  • Myelosuppression
  • mucosal toxicity
  • central nervous system toxicity
  • graft versus host disease
  • haemorrhage
  • heart failure
  • hepatic disorders
  • intracranial aneurysm
  • intracranial haemorrhage
  • multi organ failure
  • increased risk of infection
  • infertility
  • chromosomal damage
  • mutagenic potential
  • carcinogenic potential
  • neurotoxic symptoms (coma, seizures with high doses)
  • High toxicity

Drug interactions

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Busulfan
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Carboplatin
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Carmustine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Chlorambucil
Severe
Database

Clinical effect not specified

Source: DDInter

Cisplatin
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Cladribine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clozapine
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cyclophosphamide
Severe
Database

.

Source: DDInter

Deferiprone
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Alkylating Agent drugs

Ask House about Thiotepa

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-10 · House clinical team