Close

What are ADC's

Our services

ADC Review
is made possible by:




Centanamycin (ML-970; indolecarboxamide)

Chemical name: N-[4-Amino-1-(2-chloroethyl)-2-naphthyl]-5,6,7-trimethoxy-1H-indole-2-carboxamide

Centanamycin, also known as  ML-970, AS-I-145 and NSC 716970, is an indolecarboxamide synthesized as a less toxic analog of CC-1065 and duocarmycin, a natural product that binds the A-T-rich DNA minor groove and alkylates DNA.

The compound, an analog of CC-1065 (a DNA minor-groove binding agent) is under preclinical investigation as a novel anticancer agent. Centanamycin has potent in vitro and in vivo cytotoxic activity, with an average GI(50) of 34 nM.  Studies have shown that centanamycin is relatively stable in plasma, being largely intact after an 8-h incubation in mouse plasma at 37°C. The compound was extensively bound to plasma proteins.

Centanamycin is only minimally metabolized by the enzymes present in S9 preparation and is not appreciably excreted in the urine or feces.   In research studies the solution formulation provided higher C(max), AUC, F values, and greater bioavailability, although the suspension formulation resulted in a later T(max) and a slightly longer T(1/2).


See: ADC Review / Knowledge Center


References:
[1] Rayburn E, Wang W, Li M, Zhang X, Xu H, Li H, Qin JJ, Jia L, Covey J, Lee M, Zhang R. Preclinical pharmacology of novel indolecarboxamide ML-970, an investigative anticancer agent. Cancer Chemother Pharmacol. 2012 Jun;69(6):1423-31. doi: 10.1007/s00280-012-1851-9. Epub 2012 Feb 25.
[2] Rayburn E, Wang W, Grau S, Li H, Xu H, Zhang X, Li M, Sommers C, Jia L, Lee M, Zhang R. Abstract 3605: Enterohepatic circulation of indolecarboxamide ML-970 (NSC 716970), an investigative anticancer agent. Proceedings: AACR 101st Annual Meeting 2010‐‐ Apr 17‐21, 2010; Washington, DC Published in Cancer Res April 15, 2010 70; 3605


Last Editorial Review: March 16, 2015

Copyright © 2015 InPress Media Group. All rights reserved. Republication or redistribution of InPress Media Group content, including by framing or similar means, is expressly prohibited without the prior written consent of InPress Media Group. InPress Media Group shall not be liable for any errors or delays in the content, or for any actions taken in reliance thereon. ADC Review / Journal of Antibody-drug Conjugates is a registered trademarks and trademarks of InPress Media Group around the world.

Add to Flipboard Magazine.

Share

Recommended Articles

Four Ways to Show Nonobviousness of ADC Inventions

05 October, 2018

When the first antibody-drug conjugate (ADC) was approved by the U.S. Food and Drug Administration (FDA) in 2000,[1] only a handful of patent applications claiming ADCs had been published.[2] As research cont...


Skip to toolbar