Synonyms: Hycamtin® | SK-S-104864-A
topotecan is an approved drug (EMA and FDA (1996))
Compound class:
Synthetic organic
Comment: Topotecan is a semisynthetic analogue of the natural plant alkaloid camptothecin (PubChem CID 24360). Camptothecin was first isolated from the bark and stem of Camptotheca acuminata, the Chinsese happy tree. Topotecan is an anticancer drug which causes DNA strand breaks and leads to cell-cycle arrest and cell death.
Marketed formulations may contain topotecan hydrochloride (PubChem CID 60699). Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖View more information in the IUPHAR Pharmacology Education Project: topotecan |
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No information available. |
Summary of Clinical Use |
Topotecan is a antineoplastic/chemotherapeutic agent used to treat metastatic ovarian cancer, relapsed or advanced cervical cancer (with cisplatin) and relapsed small cell lung cancer. |
Mechanism Of Action and Pharmacodynamic Effects |
Topotecan works in an identical manner to camptothecin. It inhibits the topoisomerase I enzyme (TOP1). This leads to breaks in the DNA strand and the DNA damage targets the cell to the apoptotic pathway. |
External links |
For extended ADME data see the following: Electronic Medicines Compendium (eMC) Drugs.com European Medicines Agency (EMA) |