Topotecan

Topotecan
Clinical data
Pregnancy; category	D (Au, U.S.);
Routes of; administration	Intravenous infusion, oral
ATC code	L01XX17 (WHO) ;
Legal status
Legal status	US: WARNING; ℞-only (U.S.), POM (UK);
Pharmacokinetic data
Bioavailability	NA
Protein binding	35%
Metabolism	Hepatic
Elimination half-life	2-3 hours
Excretion	Renal
Identifiers
	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;
CAS Number	123948-87-8 119413-54-6 (hydrochloride);
PubChem CID	6419854;
DrugBank	APRD00687;
CompTox Dashboard (EPA)	DTXSID3042685 ;
ECHA InfoCard	100.213.372
Chemical and physical data
Formula	C23H23N3O5 •HCl
Molar mass	Expression error: Unexpected < operator457.9 g/molExpression error: Unexpected < operator

Topotecan hydrochloride (trade name Hycamtin) is a chemotherapy agent that is a topoisomerase I inhibitor. It is the water-soluble derivative of camptothecin. 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.

Indications (Approved uses)

Ovarian cancer (FDA May 1996).^[2]
Cervical cancer (FDA June 2006).^[3] ^[4]
Small cell lung cancer (SCLC) (FDA Oct 2007).^[5] ^[6]

Experimental use

Administration

IV, oral.

Mode of action

Topotecan acts by forming a stable covalent complex with the DNA/topoisomerase I aggregate, the so-called 'cleavable complex'. This process leads to breaks in the DNA strand resulting in apoptosis.

Side effects

Diarrhea
Low blood counts
Susceptibility to infection

References

External links

This pharmacology-related article is a stub. You can help Wikipedia by expanding it.

[FDA-AllBoxedWarnings-1] "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 Oct 2023.

[2] ttp://www.fda.gov/bbs/topics/NEWS/NEW00537.html

[3] ttp://www.cancer.gov/cancertopics/druginfo/fda-topotecan-hydrochloride

[4] ttp://www.fda.gov/CDER/Offices/OODP/whatsnew/topotecan.htm FDA

[5] ttp://onctalk.com/2007/12/18/oral-topotecan-fda-approved/

[6] ttp://www.drugs.com/newdrugs/gsk-receives-approval-hycamtin-topotecan-capsules-relapsed-small-cell-lung-cancer-671.html Press release

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