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Recognition and Evaluation of Lapachol as an Antitumor Agent^1,2,

The John L. Smith Memorial for Cancer Research, Chas. Pfizer & Co., Inc., Maywood, New Jersey 07607

The extracts of Stereospermum suaveolens showed reproducible activity against the Walker 256 intramuscular tumor system. The active principle was isolated and shown to be identical with the known compound lapachol, 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthoquinone. Lapachol shows highly significant activity against Walker 256 carcinosarcoma when given by intraperitoneal, subcutaneous, intramuscular, and oral routes. The best activity and therapeutic index are shown when the drug is given twice daily by the oral route.

¹ This study was supported by Research Contract PH 43-64-50 from the National Cancer Institute, Cancer Chemotherapy National Service Center, NIH, Bethesda, Maryland.

² Presented in part at the American Association for Cancer Research Meetings in April 1967 at Chicago, Illinois.

Received 2/ 6/68. Accepted 5/ 1/68.