Drug intelligence / Profile preview

valrubicin

Development stage
Approved
Lead developer
Endo International
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravesical
01

Overview

Valrubicin is a semisynthetic analog of the anthracycline doxorubicin, classified as an anthracycline antitumor antibiotic and used as a chemotherapy agent. It is administered intravesically (directly into the bladder) for the treatment of Bacillus Calmette-Guerin (BCG)-refractory carcinoma in situ (CIS) of the urinary bladder in patients for whom immediate cystectomy would be associated with unacceptable morbidity or mortality. Its mechanism of action involves interference with nucleic acid metabolism, including inhibition of nucleoside incorporation into nucleic acids, induction of chromosomal damage, cell cycle arrest at G2 phase, and—primarily through its metabolites—inhibition of DNA topoisomerase II's normal breaking-resealing function[3][6][8]. Valrubicin was originally launched under the brand name Valstar in 1999 and is approved for use in BCG-resistant non-muscle invasive bladder cancer[7].

Brand names
Valstar
02

Targets

DNATOP2A (DNA topoisomerase II)

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