PNU-159682, an active nemorubicin metabolite, is a highly potent anthracycline toxin that retains antitumor activity in vivo. Similarly to other anthracyclines PNU-159682 intercalates between the CG base pairs of DNA, but the stability of the complexes is much higher.
Clinical cancer research : an official journal of the American Association for Cancer Research, 11(4), 1608-1617 (2005-03-05)
Nemorubicin (3'-deamino-3'-[2''(S)-methoxy-4''-morpholinyl]doxorubicin; MMDX) is an investigational drug currently in phase II/III clinical testing in hepatocellular carcinoma. A bioactivation product of MMDX, 3'-deamino-3'',4'-anhydro-[2''(S)-methoxy-3''(R)-oxy-4''-morpholinyl]doxorubicin (PNU-159682), has been recently identified in an incubate of the drug with NADPH-supplemented rat liver microsomes. The aims
The antitumor anthracycline nemorubicin is converted by human liver microsomes to a major metabolite, PNU-159682 (PNU), which was found to be much more potent than its parent drug toward cultured tumor cells and in vivo tumor models. The mechanism of
Molecular cancer therapeutics, 16(5), 879-892 (2017-03-05)
Antibody-drug conjugates (ADC) are highly potent and specific antitumor drugs, combining the specific targeting of mAbs with the potency of small-molecule toxic payloads. ADCs generated by conventional chemical conjugation yield heterogeneous mixtures with variable pharmacokinetics, stability, safety, and efficacy profiles.
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