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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ALKYLATING AGENTS › Ethylene imines
thiotepa
L01AC01
Forms & Strengths
- Injectable powder for reconstitution: 15 mg
- Intravenous solution: 100 mg/10 mL
Adult Dosing
- Intravenous/Intracavitary: 0.3-0.4 mg/kg IV every 1 to 4 weeks
- High-dose conditioning regimen for hematopoietic stem cell transplantation: 500 mg/m² to 900 mg/m² total dose divided over 2 to 3 days
- Intravesical: 60 mg in 30-60 mL distilled water weekly for 4 weeks for superficial bladder carcinoma
Pediatric Dosing
- Hematopoietic stem cell transplantation conditioning: Dosing varies significantly by institutional protocols, typically ranging from 150 mg/m²/day to 375 mg/m²/day for 2 to 4 days
- Safety and efficacy in pediatric patients for indications other than conditioning regimens have not been firmly established
Indications
- Adenocarcinoma of the breast
- Adenocarcinoma of the ovary
- Superficial papillary carcinoma of the urinary bladder
- High-dose chemotherapy conditioning prior to allogeneic or autologous hematopoietic stem cell transplantation
Mechanism of Action
- Bifunctional alkylating agent that produces cross-linking of DNA strands
- Inhibits DNA, RNA, and protein synthesis by releasing ethylenimino groups that covalently bind to DNA bases
Contraindications
- Hypersensitivity to thiotepa
- Severe bone marrow suppression (unless clinically warranted for transplant conditioning)
- Pregnancy and lactation due to teratogenic and mutagenic risks
Adverse Reactions
- Severe myelosuppression (leukopenia, thrombocytopenia, anemia)
- Amenorrhea, azoospermia, and gonadal suppression
- Mucositis, stomatitis, nausea, vomiting, and diarrhea
- Hepatic veno-occlusive disease (especially in high-dose transplant regimens)
- Central nervous system toxicity (dizziness, headache, confusion with high doses)
- Bladder irritation, dysuria, and hematuria (with intravesical administration)
Drug Interactions
- Concomitant live vaccines may potentiate vaccine-induced viral replication and increase adverse reactions
- Other myelosuppressive agents and radiation therapy increase the risk of severe bone marrow suppression
- CYP450 inhibitors or inducers may theoretically alter metabolism, though thiotepa is primarily cleared via spontaneous and enzymatic pathways
Curated Content: Needs Vetting Before Put to Clinical Use