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CIBA-GEIGY AND PARKE-DAVIS JOIN RACE TO DEVELOP NEXT GENERATION OF ACE INHIBITORS: DRUG CLASS HAS FOUR NEW LISTINGS IN 1986 USAN AND USP DICTIONARY OF DRUG NAMES

Executive Summary

Ciba-Geigy and Parke-Davis have joined the race with Squibb and Merck to bring to market the next generation of angiotensin converting enzyme (ACE) inhibitors. Ciba-Geigy's pentopril and Parke-Davis' quinapril, are among the compounds appearing for the first time in the recently released 1986 edition of the USAN and USP Dictionary of Drug Names. In addition, USV's pivopril and Squibb's zofenapril are also listed for the first time. Overall, 89 new human pharmaceutical compounds -- out of a total of 107 new chemical compound listings -- appear in the USP dictionary for the first time. The total number of new listings is approximately double the roughly 50-60 new drug listings that have appeared in each new edition of the reference book over the last five years. (For a full run-down of new names in the 1986 USAN and USP dictionary,s ee chart, pp. 5 & 6) Squibb, Parke-Davis, USV, and Ciba-Geigy are among the swelling ranks of companies seeking to come up with an ACE inhibitor to compete with Squibb's Capoten (captopril), the only drug of the class to have reached the market, and Merck's Vasotec (enalapril), which could reach the market by the end of 1985. In order to build on their initial market entries, both Merck and Squibb are developing second generation ACE inhibitors. Both Merck's lisinopril and Squibb's zofenopril have reached Phase III clinicals. Marketed with limited indications in hypertension since 1981, and later in congestive heart failure, Capoten generated worldwide sales of $174 mil. in 1984, including $74 mil. in U.S. sales. Pharmaceutical Data Services recently predicted that U.S. retail pharmacy sales of Capoten would top $110 mil. at acquisition cost in 1985 ("The Pink Sheet" July 1, T&G-7). New labeling for Capoten covering all degrees of hypertension was approved by FDA in early July. Among the potential challengers to Squibb, Parke-Davis has reported that it has three ACE inhibitors in the pipeline -- indolapril and quinapril in Phase II studies and CI-925 in Phase I/II> USV said its ACE inhibitor pivopril, although an active developmental compound, has been deemphasized as a research priority. Ciba-Geigy's pentopril is still in preclinical evaluation. In addition, Schering and Wyeth have thrown their hats into the ring. Schering's SCH-338W is in Phase II clinicals. Wyeth reported at an analysts meeting in June that it has an ACE inhibitor compound approaching clinical study. In all cardiovascular compounds listed in the reference book for the first time numbered 24, or approximately one of four new drug listings. Among this group were 15 compounds in drug classes with potential use in the treatment of hypertension. In addition to the four ACE inhibitors listed for the first time, the new edition of the USAN dictionary also includes two new calcium blockers (Roche's tiapamil and Fujisawa's nilvadipine), two alpha blockers (Synthelabo's alfuzosin and Wyeth's indoramin), and two beta blockers (Synthelabo's cicloprolol and American Critical Care's flestolol). The compilation of new listings also includes Rorer's vasodilator biclodil (formerly WHR-1051B), Hoechst-Roussel's diuretic brocrinat, and three drugs listed as "antihypertensives": Lilly's quinpirole, Upjohn's losulazine, and Sterling's ofornine. New listings in the USAN for congestive heart failure drugs include three cardiotonic agents: Ayerst's pelrinone; Merrell Dow's piroximone; and Roche's quazinone. However, Roche's quazinone development project in the U.S. has been discontinued, the firm said. Ayerst has reported that pelrinone is in Phase II evaluation. After cardiovasculars, the therapeutic area with the most new drug listings in the 1986 USAN and USP dictionary is the anti-inflammatory/analgesic area with 13 new listings, including 10 first-time compounds. Psychopharmacologicals, including antidepressants, antipsychotics, and tranquilizers, is the next largest group of new listings with 11, followed by allergy/asthma/antihistaminic agents (nine listings), antibacterials (nine listings), central nervous system agents (five listings), anti-virals (three listings), and anticancer and anti-malaria agents with two listings each. Of those companies with newly listed human pharmaceutical compounds in the USAN and USP dictionary, J&J led all firms with ten new compounds. In addition, the antibacterial ofloxacin is listed under the drug's discoverer, Daiichi Seiyaku, which has licensed the drug to J&J. The dictionary indicates that Janssen continues to flourish as a drug discovery center. The list of new J&J listings includes seven Janssen compounds, two Ortho compounds and a McNeil anti-cancer compound, fenretinide, now in clinicals. Of the Janssen compounds listed, the antifungal itraconozole and the anxiolytic ritanserin are in clinicals in the U.S. Another anxiolytic, altanserin, and the antihistaminic levocabastine are active IND compounds in Europe, but are not in development in the U.S. Ortho's LHRH agonist histrelin is currently in clinicals. However, the antiviral edoxudine, although an IND drug, is inactive, the firm said. Following J&J in the number of new listings in the 1986 edition are American Home Products and Upjohn, each with eight listings. Roche led all foreign firms with seven new listings, including its monobactam antibiotic carumonam, the antibacterial coumermycin, the antimalarial mefloquine, the antidepressant piquindone, the anti-asthma/anti-allergy agent tiacrilast, quazindone, and the calcium channel blocker tiapamil. Except for quazinone, Roche indicated that all of the newly listed drugs are in clinicals in the U.S. After Roche, a number of new listings are Sterling (five new listings), Pfizer, Syntex and Burroughs Wellcome (four new listings each), and Fisons, Ciba-Geigy, and Synthlabo (three listings each). The preface to the USP dictionary explains that a USAN (U.S. adopted name) listed "originates from a firm or an individual who has developed a substance of potential therapeutic utility to the point where there is a distinct possibility of its being marketed in the U.S." The preface adds that "the process of selecting a USAN should be initiated preferably during the period of investigation when the substance is under clincal study in human and animal subjects, so that the adoption of the USAN will be complete by the time the relevant NDA is filed." However, initial listing in the USAN and USP dictionary does not necessarily mean that a drug is in the pre-NDA stage. Janssen's Sufenta (sufentanil), Merrell Dow's Nicorette (nicotine polacrilex), Mission Pharmacal's Calcibind (cellulose sodium phosphate), and Unimed's Marinol (dronabinol) are all listed for the first time in the 1986 edition of the USAN and USP dictionary even though each of these products has been approved. Also, listed drugs may represent inactive or discontinued research projects. The 1986 edition includes 2,335 listings for U.S. adopted names for pharmaceutical compounds released from June 15, 1961 through June 15, 1985 and 4,764 international nonproprietry names published by the World Health Organization from 1953 through 1984. For the first time, the 1986 edition also includes a separate section listing international nonproprietary names for drugs not currently recognized in the U.S. The dictionary is available from the U.S. Pharmacopeial Convention for $54.95. Copies may be obtained by writing USP at 12601 Twinbrook Parkway, P.O. Box 2248, Rockville, Md. 20852.
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