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Topotecan
drug data and news
Topotecan drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Topotecan | ||
| Brand Names/Synonyms | Hycamptamine; Hycamptin; Hycamtin; TOPOTECAN, HYCAMTIN; TPT; TTC; Topotecan; Topotecan Hcl; Topotecan Hydrochloride; Topotecan Lactone; Topotecane [Inn-French]; Topotecanum [Inn-Latin] | ||
| Indication | For the treatment of metastatic carcinoma of the ovary and small cell lung cancer following the failure of first-line chemotherapy. | ||
| Sponsored links | Description | Not Available | |
| Pharmacology | Topotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. Topotecan interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells may also be affected by the medicine, other effects may also occur. Unlike irinotecan, topotecan is found predominantly in the inactive carboxylate form at neutral pH and it is not a prodrug. | ||
| Mechanism Of Action | Topotecan has the same mechanism of action as irinotecan. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. The cytotoxicity of topotecan is thought to be due to double strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topotecan, topoisomerase I and DNA. Mammalian cells cannot efficiently repair these double strand breaks. | ||
| Topotecan News (When available) |
CA-125 May Not Be Reliable Marker for Response to Doxil® In ... May 3, 2006 Hana Biosciences Completes Licensing of Three Targeted Cancer Drug ... May 8, 2006 Inex Pharmaceuticals Closes Hana Biosciences Licensing Agreement May 8, 2006 Hycamtin® More Convenient than Etoposide in Small Cell Lung ... May 5, 2006 Genetic insights may explain retinal growth, eye cancer May 10, 2006 Hana Biosciences Reports First Quarter 2006 Results May 4, 2006 Lung cancer CPT-11/SN-38 resistance marked by ABCG2 expression Apr 20, 2006 | ||
| Dosage Forms | POWDER FOR SOLUTION | ||
| Drug_Category | Antineoplastic Agents; Enzyme Inhibitors; ATC:L01XX17 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Topotecan: Pharmacokinetic studies of the interaction of topotecan with concomitantly administered medications have not been formally investigated. In vitro inhibition studies using marker substrates known to be metabolized by human P450 CYP1A2, CYP2A6, CYP2C8/9, CYP2C19, CYP2D6, CYP2E, C.P.A. or CYP4A or dihydropyrimidine dehydrogenase indicate that the activities of these enzymes were not altered by topotecan. Enzyme inhibition by topotecan has not been evaluated in vivo. Concomitant administration of G-CSF can prolong the duration of neutropenia, so if G-CSF is to be used, it should not be initiated until day 6 of the course of therapy, 24 hours after completion of treatment with Hycamtin . Myelosuppression was more severe when Hycamtin was given in combination with cisplatin in Phase I studies.
In a reported study on concomitant administration of cisplatin 50 mg/m2 and Hycamtin at a dose of
1.25 mg/m2/day x 5 days, one of three patients had severe neutropenia for 12 days and a second patient
died with neutropenic sepsis. There are no adequate data to define a safe and effective regimen for Hycamtin
and cisplatin in combination. | ||
| Toxicity | The primary anticipated complication of overdosage would consist of bone marrow suppression. | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | (S)-10-[(dimethylamino) methyl]-4-ethyl-4,9-dihydroxy-1H-pyrano[3', 4' | ||
| Chemical Formula | C23H23N3O5 | ||
| Molecular Weight | 421.446 g/mol | ||
| Smiles String | CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C3=C2)N=C5C=CC(=C(C5=C4)CN(C)C)O)O | ||
| Melting Point | 213-218 °C | ||
| Water Solubility | 1 mg/ml | ||
| State | Solid (light yellow to greenish powder) | ||
| LogP/Hphobicity | 1.21 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Topotecan undergoes a reversible pH dependent hydrolysis of its lactone moiety; it is the lactone form that is pharmacologically active. | ||
| Half Life | 2-3 hours | ||
| Protein Binding [%] | 35% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Topotecan.html http://www.rxlist.com/cgi/generic2/topotec.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00687 | ||
| CAS Registry Number | 119413-54-6 | ||
| KEGG Compound ID | C11158 | ||
| PubChem ID | SID:606579 | ||
| PharmGKB ID | PA451729 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2231116 |
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