Topotecan

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Topotecan
Systematic (IUPAC) name
(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
Identifiers
CAS number	123948-87-8 119413-54-6 (hydrochloride)
ATC code	L01XX17
PubChem	6419854
DrugBank	APRD00687
Chemical data
Formula	C₂₃H₂₃N₃O₅ •HCl
Mol. mass	457.9 g/mol
Pharmacokinetic data
Bioavailability	NA
Protein binding	35%
Metabolism	Hepatic
Half life	2-3 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	D (Au, U.S.)
Legal status	℞-only (U.S.), POM (UK)
Routes	Intravenous infusion, oral

Topotecan hydrochloride (trade name Hycamtin) is a chemotherapy agent that is a topoisomerase 1 inhibitor. It is used to treat ovarian cancer and lung cancer, as well as other cancer types.

After GlaxoSmithKline received final FDA approval for Hycamtin Capsules on October 15, 2007, Topotecan is the first topoisomerase inhibitor for oral use.

[edit] Administration

IV, oral.

[edit] Side effects

Diarrhea
Low blood counts
Susceptibility to infection

[edit] External links

v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)

Alkylating and alkylating-like agents	Nitrogen mustards: (Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan, Bendamustine, Uramustine) Nitrosoureas:(Carmustine, Fotemustine, Lomustine, Streptozocin) Platinum (alkylating-like): (Carboplatin, Cisplatin, Oxaliplatin, Triplatin tetranitrate, Satraplatin) Alkyl sulfonates:(Busulfan, Treosulfan) Hydrazines:(Procarbazine, Dacarbazine, Temozolomide) Aziridines:(ThioTEPA)

Antimetabolites	Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine) Pyrimidine:(Capecitabine, Cytarabine, Decitabine, Fluorouracil, Floxuridine, Gemcitabine)

Spindle poison/mitotic inhibitor	Taxane: (Docetaxel, Larotaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).

Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Pixantrone, Valrubicin) streptomyces (Actinomycin, Bleomycin, Mitomycin, Plicamycin) - Hydroxyurea

Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan, Rubitecan), Podophyllum:(Etoposide, Teniposide)

CI monoclonal antibodies	Receptor tyrosine kinase (Cetuximab, Panitumumab, Trastuzumab) - CD20 (Rituximab, Tositumomab) - other (Alemtuzumab, Bevacizumab, Gemtuzumab)

Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin

Tyrosine kinase inhibitors	Axitinib, Bosutinib, Cediranib, Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Lestaurtinib, Nilotinib, Semaxanib, Sorafenib, Sunitinib, Vandetanib

Cyclin-dependent kinase inhibitor	Seliciclib

Other	retinoids (Alitretinoin, Tretinoin), Fusion protein (Aflibercept) - Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase (Pegaspargase), Bexarotene, Bortezomib, Celecoxib, Denileukin diftitox, Elesclomol, Estramustine, Irofulven, Ixabepilone, Masoprocol, Mitotane, Oblimersen, Testolactone, Tipifarnib, Trabectedin