Camptothecin

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Camptothecin
Systematic (IUPAC) name
4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b] quinoline-3,14-(4H,12H)-dione
Identifiers
CAS number	7689-03-4
ATC code	?
PubChem	2538
Chemical data
Formula	C₂₀H₁₆N₂O₄
Mol. mass	348.352 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
Routes	?

Camptothecin is a plant secondary metabolite used as an anti-cancer drug that damages DNA, leading to the destruction of the cell.

It comes from Camptotheca acuminata, a deciduous tree found in southern China. Stem woods of Nothopodytes foetida (previously known as Mappia foetida) found in the western ghats of India are an even better source of camptothecin.^{[citation needed]} A close analogue, 9-methoxycamptothecin, is also present in the same source.

1 Mechanism of action
2 Related medications
3 References
4 External links

[edit] Mechanism of action

Camptothecin affects the activity of the enzyme topoisomerase I, whose normal action is to cleave, unwind, and religate DNA. ^[1]

When camptothecin binds to topoisomerase I, it will be able to cleave but not to religate DNA. Thereby, camptothecin causes single strand breaks in DNA.

[edit] Related medications

Topotecan (trade name Hycamtin) and irinotecan {trade name Camptosar, also known as CPT-11) are camptothecin derivatives marketed as anti-cancer drugs by GlaxoSmithKline and Pfizer, respectively. Topotecan is indicated for small cell lung cancer after failure of first-line chemotherapy and metastatic carcinoma of the ovary following failure of initial or subsequent chemotherapy. Irinotecan is indicated for colorectal cancers and is usually taken with other drugs in chemotherapy.

[edit] References

^ Capranico G, Ferri F, Fogli M, Russo A, Lotito L, Baranello L (2007). "The effects of camptothecin on RNA polymerase II transcription: Roles of DNA topoisomerase I". Biochimie. PMID 17336444.

[edit] External links

Camptothecin Project From the Stehlin Foundation for Cancer Research

Pfizer Oncology From Pfizer Oncology

GlaxoSmithKline From GlaxoSmithKline

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v • d • e Chemotherapeutic agents/Antineoplastic agents (L01)
Alkylating agents	Nitrogen mustards: (Chlorambucil, Chlormethine, Cyclophosphamide, Ifosfamide, Melphalan). Nitrosoureas:(Carmustine, Fotemustine, Lomustine, Streptozocin). Platinum: (Carboplatin, Cisplatin, Oxaliplatin, BBR3464). Busulfan, Dacarbazine, Mechlorethamine, Procarbazine, Temozolomide, ThioTEPA, Uramustine
Antimetabolites	Folic acid: (Aminopterin, Methotrexate, Pemetrexed, Raltitrexed). Purine:(Cladribine, Clofarabine, Fludarabine, Mercaptopurine, Pentostatin, Thioguanine). Pyrimidine:(Capecitabine, Cytarabine, Fluorouracil, Floxuridine, Gemcitabine)
Spindle poison plant alkaloids	Taxane: (Docetaxel, Paclitaxel). Vinca: (Vinblastine, Vincristine, Vindesine, Vinorelbine).
Cytotoxic/antitumor antibiotics	Anthracycline family: (Daunorubicin, Doxorubicin, Epirubicin, Idarubicin, Mitoxantrone, Valrubicin). Bleomycin, Hydroxyurea, Mitomycin, Actinomycin
Topoisomerase inhibitors	Camptotheca: (Camptothecin, Topotecan, Irinotecan), Podophyllum:(Etoposide, Teniposide).
CI monoclonal antibodies	Alemtuzumab, Bevacizumab, Cetuximab, Gemtuzumab, Panitumumab, Rituximab, Tositumomab, Trastuzumab
Photosensitizers	Aminolevulinic acid, Methyl aminolevulinate, Porfimer sodium, Verteporfin
Kinase inhibitors	Dasatinib, Erlotinib, Gefitinib, Imatinib, Lapatinib, Nilotinib, Sorafenib, Sunitinib, Vandetanib (ZD6474)
Other	Alitretinoin, Altretamine, Amsacrine, Anagrelide, Arsenic trioxide, Asparaginase, Bexarotene, Bortezomib, Denileukin diftitox, Estramustine, Hydroxycarbamide, Masoprocol, Mitotane, Pegaspargase, Tretinoin