N-acetylmelphalan

07/01/1988 - "This and other experiments indicated that the antitumor effect and tumor localization of N-AcMEL-MoAb conjugates can be enhanced in vivo by rTNF-alpha, thereby enabling successful eradication of larger established subcutaneous murine tumors."
01/01/1987 - "In addition, N-AcMEL-MoAb conjugates more effectively erradicated tumors in vivo than does free MEL or N-AcMEL. "
01/01/1987 - "To overcome these nonspecific effects N-acetyl melphalan (N-AcMEL) was synthesized and found to be 75 times less toxic to tumor cells in vitro. "
07/01/1988 - "To potentiate the antitumor effect of the N-AcMEL-MoAb conjugate, studies were undertaken to analyze its action in combination with recombinant human tumor necrosis factor alpha (rTNF-alpha), a monokine, capable of causing acute necrosis of syngeneic tumor transplants in mice. "
09/01/1989 - "Melphalan (MEL), an alkylating agent, has been modified to a derivative, N-acetylmelphalan (N-AcMEL), which can be conjugated to anticolon cancer monoclonal antibodies (MoAbs 30.6, I-1, and JGT) and used for immunochemotherapy. "

07/01/1988 - "To potentiate the antitumor effect of the N-AcMEL-MoAb conjugate, studies were undertaken to analyze its action in combination with recombinant human tumor necrosis factor alpha (rTNF-alpha), a monokine, capable of causing acute necrosis of syngeneic tumor transplants in mice. "

09/01/1989 - "In a phase I clinical study, N-AcMEL-MoAb conjugates were administered via the hepatic artery to 10 patients, nine of whom had disseminated colorectal cancer (including the liver) and one of whom had Dukes' C colon cancer that had been resected. "
12/01/1990 - "Human anti-mouse antibody (HAMA) response was determined in the serum of 67 patients who received subcutaneously administered radiolabelled murine monoclonal antibodies (MoAb) (50 micrograms-3 mg) for immunolymphoscintigraphy and of 10 patients with advanced colorectal cancer who received murine MoAb-N-acetyl melphalan (MoAb-N-AcMEL) conjugates (amount of MoAb ranged from 120 mg/m2 body surface area to 1000 mg/m2 body surface area) as therapy. "

07/01/1988 - "N-Acetyl-melphalan-MoAb (N-AcMEL-MoAb) conjugates have previously been shown to have greater antitumor activity than N-AcMEL, melphalan, or MoAb alone against both subcutaneous and ascites murine thymomas in mice (1). "

12/01/1990 - "Further administration of MoAb-N-AcMEL conjugates to a patient, who had already developed HAMA, led to 'serum sickness'-type symptoms and a transient reduction in the HAMA titres. "