Summary
Ethylbis(2,2-dimethyl-1-aziridinyl)phosphinate (AB-163) was used to treat 27 patients in a phase I trial. The limiting toxicity on a weekly schedule of IV administration involved nausea and vomiting associated with a variety of cholinergic side effects, including possible seizures. A starting dose of 300–400 mg/M2/week is suggested for a Phase II trial. One partial response in a patient with squamous-cell carcinoma of the cervix metastatic to the lungs was seen.
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References
Bardos TJ (1962) Consideration of chemical reaction mechanisms in relationship to the biological action of dual antagonists. Biochem Pharmacol 11:256–260
Bardos TJ (1979) Chemical mechanisms of the radiation potentiating effects of 2,2-dimethylaziridine-type antitumor agents. Internat J Radiat Oncol Biol Phys 5:1653–1656
Bardos, TJ, Olsen DB, Enkoji T (1957) Synthesis of deoxyalloxazines (benzopteridines). J Am Chem Soc 79:4704–4708
Bardos TJ, Papanastassiou ZB, Segaloff A, Ambrus JL (1959) Dual antagonists: Alkyl N-bis(ethylenimido)phosphorocarbamates. Nature 183:399–400
Bardos TJ, Ambrus JL, Ambrus CM (1971) Combination of chemotherapy with dual antagonists and radiotherapy in the treatment of neoplastic disease. J Surg Oncol 3:431–441
Chmielewicz ZF, Bardos TJ, Munson A, Babbitt H, Ambrus JL (1967) Synthesis and chemotherapeutic effects of ethyl bis-(2,2-dimethyl)-ethylenamido phosphate: A preliminary report. J Pharm Sci, 56:1179–1181
Munson AE, Babbitt H, Chmielewicz ZF, Bardos TJ, Ambrus JL (1969) Studies on the chemistry, antitumor activity and pharmacology of ethyl di-(2,2-dimethyl)ethylenamido phosphate (AB-163). J Surg Oncol 1:167–180
Regelson W, Pierucci O (1964) The effect of radiation on splenomegaly induced by the Friend leukemia virus and its modification by ethyl-N-bis(2,2-dimethyl-ethylamidinophosphoro)-carbamate (AB-132), actinomycin D, and AET. Radiat Res 22:368–381
Wampler GL, Regelson W, Bardos TJ (1978) Absence of cross resistance of alkylating agents in cyclophosphamide resistant L1210 leukemia. Eur J Cancer 14:977–982
Wampler GL, Belgrad R, Wassum JA (1979) Radiation potentiating effect of ethyl bis(2,2-dimethyl-1-aziridinyl)phosphinate (AB-163). Internat J Radiat Oncol Biol Phys 5:1681–1683
Wodinsky I, Swiniarski J, Kensler CJ, Venditti JM (1974) Combination radiotherapy and chemotherapy for P388 lymphocytic leukemia in vivo. Cancer Chemother Rep [2] 4:73–97
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Formerly ethylbis-(2,2-dimethyl)-ethylenamido phosphate (NSC 108878)
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Wampler, G.L., Kuperminc, M. & Regelson, W. Phase I study of ethylbis(2,2-dimethyl-1-aziridinyl)phosphinate (AB-163). Cancer Chemother. Pharmacol. 4, 49–52 (1980). https://doi.org/10.1007/BF00255459
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DOI: https://doi.org/10.1007/BF00255459