Ayerst Laboratories

In 1982 Ayerst Laboratories in Montreal became the first company in Canada to install a commercial software tool (the SYBYL suite from Tripos Associates) to help in the development of pharmacophoric models from structure-activity relationships. The installation of the software was the second ever, worldwide, by a company and is a testimonial to the foresight of the director of medicinal chemistry, Dr. Leslie Humber, for having championed its installation. Dr. Adi M. Treasurywala, then an organic chemist with some experience in medicinal chemistry, became the first industrial computational chemist in Canada that year. The use of modeling approaches contributed in a minor but significant way to the discovery of the compound known as Tolrestat, which was an inhibitor of lens aldose reductase. This led to the acknowledgment of Treasurywala as a coinventor of the drug on several patents that were filed in this research area. Approximately in 1983, Ayerst closed down its discovery effort in Canada and moved to Princeton, New Jersey, where an expanded effort in the area of computational chemistry continues. 

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R. D. Daley, Ayerst Laboratories, Rouses Point, New York E. Debesis, Hoffmann-LaRoche, Inc., Nutley, New Jersey... 

Wyeth-Ayerst Laboratories and Immunex Inc. Etanercept (Enbrel ) Product Insert, 2006. 

FDA Wyeth-Ayerst Laboratories Announces the Withdrawal of Duract from the Market, www.fda.gov/hhs/ topics/ANSWERS/ANS00879.html, last accessed on 12fh December 2003. 

Disulfiram is the generic name for Antabuse, a drug used in the treatment of chronic alcoholism. Disulfiram potentiates the toxic and carcinogenic effects of 1,2-dibromoethane in experimental animals. Presumably, this occurs by blocking conversion of the aldehyde metabolite as with acetaldehyde from ethanol. There is no evidence that similar effects occur in humans. Based on animal data, however, Ayerst Laboratories, producers of Antabuse (disulfiram), recommended the following in the package insert "Patients taking Antabuse tablets should not be exposed to ethylene dibromide or its vapors" (PDR 1991). 

If the rat experiences respiratory problems during recovery, doxapram hydrochloride is administered (Dopram-V 0.10 cc, i.p. Ayerst Laboratories). Two days following surgery, the patency of each cannula is checked and betadine is applied to the surgical wound (10% Povidone-iodine Purdue Frederick). 

Norplant is a registered trademark of the Population Council, It is manufactured and distributed by Leiras Pharmaceuticals in Finland, under license from the Population Council, It is marketed in the United States by Wyeth-Ayerst Laboratories, Inc, of Philadelphia. 

Ayerst Laboratories, Division of American Home Products Corp., New York, N.Y. Protopam chloride (Pralidoxime chloride). Professional brochure. 1973. 39 p. 

Sirolimus (Rapamycin, Rapamune ), a natural macrocyclic lactone, is a potent immunosuppressive agent. It was developed by Wyeth-Ayerst Laboratories (Philadelphia, Pennsylvania, U.S.A.) and approved by the Food and Drug Administration for the prophylaxis of renal transplant rejection in 1999 (28,29). Sirolimus has its roots in Easter Island, where an actinomycete streptomyces hygroscopicus was found that produced a novel macrolide antibiotic with potent antibiotic, potent antifungal, immunosuppressive, and antimitotic activities. 

Rapamycin (Rapamune, Wyeth-Ayerst Laboratories) is a natural macrocyclic lactone with a potent immunosuppressive and antiproliferative effect that was approved by the Food and Drug Administration for the prophylaxis against renal transplant rejection,... 

Fenfluramine (approved in 1973, withdrawn in 1997) and phentermine (appetite suppressant approved in 1959 and still available). Wyeth-Ayerst Laboratories, a subsidiary of American Home Products Corp. of Madison, New Jersey, manufactured and marketed fenfluramine under the brand name Pondimin. Wyeth-Ayerst also marketed Redux (dexfenfluramine), which was manufactured for Interneuron Pharmaceuticals. See http //www.fda.gov/cder/news/phen/fenphenpr81597.htm... 

Redux, package insert. Wyeth-Ayerst Laboratories, Philadelphia, PA, U.S.A. 

Memorandum of meeting between FDA and Ayerst Laboratories, 10 September 1976, FDA Files, AFi 19-003, Accession 88-83-77. 

Crout, J. Richard, to H. Perdue (Ayerst Laboratories), 22 December 1974. FDA Files. AF 19-003. Accession 88-82-22. 

Fig. 1 shows the infrared spectrum of halothane (Ayerst Laboratories Inc. Batch No. 1CKB). The spectrum is that of undiluted halothane in a 0.104 mm. potassium bromide cell vs. a potassium bromide plate. Also, because some of the absorption bands are quite intense, Fig. 1 shows the spectrum of a 4.0 volume percent solution of halothane in carbon disulfide, in a 0.104 mm. potassium bromide cell, vs. a 0.1 mm. cell filled with carbon disulfide. A Beckman Model IR-12 instrument was used. Considering the variety of sample handling techniques used, this spectrum and other published spectra (1-3) are the same. 

The writer wishes to thank Mr. A. Holbrook of Imperial Chemical Industries Ltd., and Dr. B, T. Kho of Ayerst Laboratories Inc., for their careful reading of the manuscript and helpful suggestions for improvements, as well as Dr. J. M. Pryce of Imperial Chemical Industries Ltd., who provided the mass spectral and nuclear magnetic resonance information for this profile. 

Editor Leslie G. Humber, Ayerst Laboratories, Montreal, Canada Chapter 1. Antidepressants... 

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