Topotecan
- Atc Codes:L01XX17
- CAS Codes:119413-54-6#123948-87-8
- PHARMGKB ID:119413-54-6#123948-87-8
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Hycamtin, Topotecan; Belgium: Hycamtin; Bulgaria: Hycamtin; Cyprus: Hycamtin; Czech Republic: Hycamtin, Topotecan; Denmark: Hycamtin; Estonia: Hycamtin, Topotecan; Finland: Hycamtin; France: Hycamtin; Germany: Hycamtin, Topotecan; Greece: Evotopin, Hycamtin; Hungary: Hycamtin, Topotecan; Ireland: Hycamtin, Topotecan; Italy: Hycamtin; Latvia: Hycamtin, Topotecan; Lithuania: Topotecan; Luxembourg: Hycamtin; Malta: Topotecan; Netherlands: Hycamtin, Topotecan; Poland: Hycamtin; Portugal: Hycamtin, Topotecano; Romania: Hycamtin, Topotecan; Slovakia: Hycamtin, Topotecan; Slovenia: Hycamtin; Spain: Hycamtin; Sweden: Hycamtin, Topotecan; UK: Hycamtin.
North America
Canada: Hycamtin, Topotecan; USA: Hycamtin.
Latin America
Argentina: Asotecan, Hycamtin, Potekam, Tisogen, Topokebir, Topotecan; Brazil: Hycamtin; Mexico: Toranex.
Drug combinations
Chemistry
Topotecan Hydrochloride: C~23~H~23~N~3~O~5~ HCl. Mw: 457.91. (1) 1H-Pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione, 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-, monohydrochloride, (S)-; (2)(S)-10-[(Dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione monohydrochloride. CAS-119413-54-6; CAS-123948-87-8 (topotecan)(1990).
Pharmacologic Category
Other Antineoplastic Agents. Natural Source (Plant) Derivative, Camptothecin. (ATC-Code: L01XX17).
Mechanism of action
Binds to topoisomerase I and stabilizes cleavable complex so that religation of cleaved DNA strand cannot occur. This results in accumulation of cleavable complexes and single-strand DNA breaks. Topotecan acts in S phase of cell cycle.
Therapeutic use
Treatment of ovarian cancer and small cell lung cancer. Cervical cancer (in combination with cisplatin).
Pregnancy and lactiation implications
Animal studies found reduced fetal body weight, eye, brain, skull, and vertebrae malformations. May cause fetal harm in pregnant women. Use during pregnancy and lactation contraindicated.
Unlabeled use
Investigational: Treatment of non-small cell lung cancer, myelodysplastic syndrome, sarcoma (pediatrics), neuroblastoma (pediatrics), refractory solid tumors (pediatrics).
Contraindications
Hypersensitivity to topotecan or any component of the formulation. Severe bone marrow depression. Pregnancy. Breast-feeding.
Warnings and precautions
Dose-limiting toxicity is bone marrow suppression (primarily neutropenia; may also cause thrombocytopenia and anemia). Should only be administered to patients with adequate bone marrow reserves, baseline neutrophils at least 1500 cells/mm^3^ and platelet counts at least 100000/mm^3^. Diarrhea reported with oral topotecan (may be severe). Incidence of diarrhea may be higher in the elderly. Topotecan-induced neutropenia may lead to neutropenic colitis. Use with caution in renal impairment.