Amsalog - CAS 80841-48-1
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Not Intended for Therapeutic Use. For research use only.
Asulacrine isethionate is the isethionate salt of an amsacrine analogue with antineoplastic properties. Asulacrine inhibits the enzyme topoisomerase ll, thereby blocking DNA replication and RNA and protein synthesis.
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Asulacrine isethionate; CI-921.
1.A phase I trial of amsalog (CI-921) administered by intravenous infusion using a 5-day schedule.
Fyfe D1, Price C, Langley RE, Pagonis C, Houghton J, Osborne L, Woll PJ, Gardner C, Baguley BC, Carmichael J; Cancer Research Campaing Phase I/II Trials Committee. Cancer Chemother Pharmacol. 2001 Apr;47(4):333-7.
PURPOSE: Amsalog, a derivative of 9-aminoacridine, is an inhibitor of topoisomerase II. Early studies of intravenous amsalog administered either once weekly, or daily for 3 days repeated every 3 weeks, showed that myelosuppression is the dose-limiting toxicity (DLT). Phase II studies showed only limited activity in breast, head and neck, and non-small-cell lung cancer. The activity of other topoisomerase inhibitors is schedule-dependent. We therefore performed a phase I study to evaluate the use of amsalog on a more prolonged schedule.
2.Enhanced therapeutic effect of amsalog (CI-921) in combination with cisplatin in vitro and in vivo.
Elliott W1, Howard C, Roberts B, Hook K, Vincent P, Corbett T, Leopold W. Oncol Rep. 1996 Nov;3(6):1153-9.
CI-921, the 5-methyl-4-carboxamide analog of amsacrine, in combination with cisplatin produced a 6-fold better cell kill in vitro than expected based on additive effects. The combination of CI-921 and cisplatin was subsequently evaluated in three in vivo model systems: intraperitoneally (TP) and intravenously (IV) implanted P388 leukemia, and advanced stage subcutaneously (SC) implanted LC-12 squamous cell carcinoma. All drug treatments were administered IP on an intermittent treatment schedule which was optimal for both agents. Combination therapy was superior to therapy with the best single agent alone, CI-921, in all three model systems. Against IP implanted P388 leukemia, combination therapy produced greater than 8 logs of net tumor cell kill with 60-day survivors (cures). This level of activity was 50-fold greater (1.7 log) than that obtained with CI-921 alone. An IV implant of P388 leukemia was used in a confirmatory study to provide a more rigorous evaluation against disseminated disease.
3.A study of amsalog (CI-921) administered orally on a 5-day schedule, with bioavailability and pharmacokinetically guided dose escalation.
Fyfe D1, Raynaud F, Langley RE, Newell DR, Halbert G, Gardner C, Clayton K, Woll PJ, Judson I, Carmichael J. Cancer Chemother Pharmacol. 2002 Jan;49(1):1-6.
PURPOSE: Amsalog is a derivative of 9-aminoacridine. Phase I studies using intravenous (i.v.) amsalog have shown the dose-limiting toxicity (DLT) to be phlebitis and myelosuppression. Phase II studies using a variety of schedules have shown evidence of activity in patients with large-cell lung, breast, and head and neck cancers. Preclinical studies demonstrated that amsalog is active orally: a clinical study of the oral bioavailability of amsalog was therefore performed.
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CAS 80841-48-1 Amsalog

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