This Article Full Text (PDF) Alert me when this article is cited Alert me if a correction is posted Services Similar articles in this journal Similar articles in PubMed Alert me to new issues of the journal Download to citation manager Citing Articles Citing Articles via Google Scholar Google Scholar Articles by Casper, E. S. Articles by Young, C. W. Search for Related Content PubMed PubMed Citation Articles by Casper, E. S. Articles by Young, C. W.

Phase I and Pharmacological Studies of Pentamethylmelamine Administered by 24-Hour Intravenous Infusion¹

Developmental Chemotherapy [E. S. C., R. J. G., G. R. L., T. M. W., C. W. Y.] and Solid Tumor [D. P. K.] Services, Department of Medicine, and the Clinical Pharmacology Laboratory [B. R. J., C. G.], Memorial Sloan-Kettering Cancer Center, Cornell University Medical College, New York, New York 10021

A Phase I study of pentamethylmelamine (PMM) was conducted, administering the drug as a 24-hr i.v. infusion once weekly for 3 weeks. Doses ranged from 80 to 3000 mg/sq m/week. Twenty-six evaluable patients received a total of 30 courses of PMM. The median performance status of the patients was 60% (range, 40 to 90%), and the median age was 58 years (range, 43 to 72 years). The highest tolerated dose was 2000 mg/sq m/week. Nausea and vomiting were the dose-limiting toxicities; myelosuppression was neither consistent nor severe.

One objective response lasting 10 months was noted in a patient with renal cancer. Pharmacokinetic studies using [ring-¹⁴C]PMM demonstrated a postinfusion half-life of ¹⁴C of approximately 12 hr, with the majority of the radiolabel excreted in the urine. PMM was introduced as a parenteral form of hexamethylmelamine. The present schedule does not permit administration of PMM in a dose greater than the tolerated dose of hexamethylmelamine and does not appear to offer an advantage over the p.o. use of the parent compound.

¹ Supported in part by Contract 1-CM97274 from the Division of Cancer Treatment and USPHS Grant CA 05826 from the National Cancer Institute, NIH, Bethesda, Md.

² Recipient of American Cancer Society Junior Faculty Fellowship.

³ To whom requests for reprints should be addressed, at Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, N. Y. 10021.

⁴ Landrum/Karnofsky Fellow.

Received 10/ 3/80. Accepted 1/ 9/81.