Disease relevance of S-9788

• S 9788 appeared to be devoid of toxicity at its effective doses [1].
• In a panel of 14 primary cultures of human renal cell carcinomas the reversal of inherent multidrug-resistance by S 9788, a new triazinoaminopiperidine derivative, was analysed [2].

High impact information on S-9788

• We conclude that S 9788 is a novel agent capable of reversing MDR in vitro and in vivo, and whose pharmacological profile warrants its selection as a candidate drug for eventual assessment in the clinic [1].
• The activity of S 9788 depended on both the MDR cell line and the cytotoxic agent [1].
• In vitro activity of S 9788 on a multidrug-resistant leukemic cell line and on normal hematopoietic cells-reversal of multidrug resistance by sera from phase I-treated patients [3].
• In two treatment regimens (Q4D days 1, 5 and 9 and QD days 1-9), S 9788 enhanced the antitumor activity of vincristine in a dose-dependent manner, resulting in a complete circumvention of drug resistance for well-tolerated doses of S 9788 [4].
• An association between reversal and P-glycoprotein (P-170) expression suggests that S 9788 exerts its activity through P-glycoprotein [2].

Associations of S-9788 with other chemical compounds

• In combination with doxorubicin S 9788 revealed an evident reversal of multidrug resistance in 12 cell cultures [2].

Analytical, diagnostic and therapeutic context of S-9788

• The triazinoaminopiperidine derivative S 9788 is a new multidrug-resistance modulator that is currently being evaluated in phase I clinical trials [3].
• In patients treated with S 9788 as a 30-min intravenous infusion during phase I trials, a good correlation was found between the serum levels of S 9788 and the ability to reverse MDR in CCRF-CEM/VLB cells [3].
• Reversal of inherent multidrug-resistance in primary human renal cell carcinoma cell cultures by S 9788 [2].

References