MERRELL DOW's SIX NEW LISTINGS IN 1987 USAN AND USP DICTIONARY IS MOST FOR ANY COMPANY; FIRM HAS AT LEAST THREE ANTIHYPERTENSIVES IN R&D PIPELINE

Merrell Dow, with six new listings for developmental human pharmaceutical compounds, led all other companies with new listings contained in the 1987 edition of the USAN and USP Dictionary of Drug Names. Of the six compounds, five are currently in clinical development and one, the antihypertensive lofexidine, already is at the NDA pending stage at FDA. In addition to lofexidine, Merrell Dow has at least two other antihypertensive compounds under development -- medroxalol and another new listing in the USAN dictionary, tipentosin, now in Phase I. Also in the cardiovascular area, Merrell Dow has the cardiotonic agent, enoximone, in clinical development. Merrell Dow's other new listings, besides lofexidine, tipentosin, and enoximone, include the anticancer agent eflornithine, the antibacterial teicoplanin, and the bronchodilator zindotrine. All three compounds have reached the human clinical stage. Overall, 51 human pharmaceuticals -- out of a total of 65 new listings -- appear for the first time in the 1987 edition of the USAN and USP Dictionary of Drug Names. The number of new pharmaceutical compounds listed in the most recent edition of the USAN and USP dictionary is the fewest number in recent years. The 1986 edition of the reference book had 89 human drug names appearing for the first time. The total of 51 new listings for human compounds does not include five contact lens material listings and four pharmaceutic aids appearing for the first time. Nor does it include two veterinary compounds or three analogs to listed compounds. After Merrell Dow in the number of new listings in this year's USAN dictionary is Squibb with five new listings. Squibb's new listings include the topical steroid tipredane, currently in Phase III clinicals, and the firm's second generation angiotensin converting enzyme inhibitor, fosenopril, in Phase II studies. Following up on its Azactam (aztreonam) antibiotic development program, Squibb's other three listings -- gloximonam, oximonam, and oximonam sodium -- are for pro-drugs to the firm's oral monobactam antibiotic tigemonam, which is in early clinicals. Squibb also has a second generation synthetic monobactam injectable antibiotic, SQ-83360, expected to enter clinicals in three to six months, the company said ("The Pink Sheet" April 7, p. 6). An NDA for Azactam is currently pending at FDA. Squibb has predicted a 1986 approval of the injectable antibiotic. Merck/Astra and Burroughs Wellcome each have four new listings, while Hoechst-Roussel and Upjohn each have three new listings. Among the Astra drugs listed for the first time are the anti-ulcer agent omeprazole, the vasodilator felodipine, and the anticancer agent enprofylline. All three compounds are in late clinicals under the sponsorship of Merck for marketing in the U.S. Upjohn's new listings indicate the company's continuing interest in drugs to combat heart attacks. The new edition of the USAN and USP dictionary has new listings for furegrelate, a thromboxane synthetase inhibitor, and itazogrel, a platelet anti-aggregatory agent, as well as the anticancer agent menogaril. Itazogrel is in the same therapeutic category as Upjohn's developmental compound ciprostene, currently in clinicals. A listing for an Upjohn anti-atherosclerotic, timefurone, appeared for the first time in the 1985 edition of USAN; development of the compound, however, had been discontinued. The 16 new listings for cardiovascular agents far outnumbered new listings for other therapeutic areas, representing nearly one-third of all new listings for human compounds in the 1987 edition. Included in the group of new cardiovascular listings are four ACE inhibitors, three calcium channel blockers, and two cardiotonic agents. Cardiovasculars were followed by antibacterials (six new listings); anti-asthma/bronchodilators, gastro-intestinal/anti-ulcer agents, and sedative/antidepressants (four new listings each); and anticancer agents (three new listings). The preface of the USP dictionary explains that a listed USAN (U.S. adopted name) "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 clinical 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 dictionary does not necessarily mean that a drug is in the pre-NDA stage. For example, an NDA for Merrell Dow's lofexidine is currently pending at FDA. Also, listed drugs may represent inactive or discontinued research projects. The 1987 edition includes 2,400 listings for U.S. adopted names for pharmaceutical compounds released from June 15, 1961 through June 15, 1986 and 4,948 international nonproprietary names compiled by the World Health Organization from 1953 to 1985. The 1987 edition also includes a separate section listing international nonproprietary names for drugs not currently recognized in the U.S. The dictionary is available from USP for $60 (prepaid). Copies may be obtained by writing USP at 12601 Twinbrook Parkway, P.O. Box 2248, Rockville, Maryland 20852. NEW U.S. ADOPTED NAMES (USAN) INCLUDED IN THE 1987 EDITION OF USAN AND THE USP DICTIONARY OF DRUG NAMES Acrivastine (antihistaminic), Burroughs Wellcome Amfilcon A (contact lens material: hydrophilic), Applied Optics Amlodipine Maleate (anti-anginal; antihypertensive), Pfizer Astifilcon A (contact lens material: hydrophilic), Breath-O, Toray Atiprosin Maleate (antihypertensive), Ayerst Avilamycin (antibacterial), Lilly Cadexomer lodine (antiseptic; anti-ulcerative), Iodosorb, Perstop Carbotec Cilazapril (antihypertensive), Roche Cimaterol (repartitioning agent), Boehringer Ingelheim Clavulanate Potassium (b-lactamase inhibitor), component of Augmentin, Beecham Colforsin (antiglaucoma agent), Hoechst-Roussel Darodipine (antihypertensive; bronchodilator; vasodilator), Sandoz Delapril HCI (antihypertensive; angiotensin converting enzyme inhibitor), USV Duoperone Fumarate (neuroleptic), Robins Eflornithine HCI (antineoplastic; antiprotozoal), Merrell Dow Efrotomycin (veterinary growth stimulant), Merck Enoximone (cardiotonic), Merrell Dow Enprofylline (bronchodilator), Astra Felodipine (vasodilator), Astra Fosarilate (antiviral), Sterling Fosenopril Sodium (antihypertensive; angiotensin converting enzyme inhibitor), Squibb Furegrelate Sodium (thromboxane synthetase inhibitor), Upjohn Gloximonam (antibacterial), Squibb Icotidine (histamine H[2] and H[1] antagonist), Smith-Kline Isomazole HCI (cardiotonic), Lilly Itazogrel (platelet anti-aggregatory agent), Upjohn Lamotrigine (anticonvulsant), Burroughs Wellcome Linogliride (antidiabetic), McNeil Lofexidine HCI (antihypertensive), Merrell Dow Lonapalene (antipsoriatic), Syntex Loratadine (antihistaminic), Schering-Plough Lortalamine (antidepressant), Lipha, S.A. Maduramicin (anticoccidal), Cygro, American Cyanamid Menogaril (antineoplastic), Upjohn Mesalamine (anti-inflammatory), Rowasa, Rowell Methylparaben (pharmaceutic aid) Methylparaben sodium (pharmaceutic aid) Milacemide HCI (anticonvulsant; antidepressant), Continental Pharma Napamezole HCI (antidepressant), Sterling Neflumozide HCI (antipsychotic), Hoechst-Roussel Nefocon A (contact lens material: hydrophobic), Ocusil, Oculus Netobimin (veterinary anthelmintic), Schering-Plough Omeprazole (gastric acid secretory depressant), Astra Oximonam (antibacterial), Squibb Oximonam Sodium (antibacterial), Squibb Piritrexim Isethionate (antiproliferative agent), Burroughs Wellcome Propylparaben (pharmaceutic aid: antifungal) Propylparaben Sodium (pharmaceutic aid: antifungal) Quazolast (anti-asthmatic; mediator release inhibitor), USV Ramipril (antihypertensive; angiotensin converting enzyme inhibitor), Hoechst-Roussel Recainam HCI (cardiac depressant; anti-arrhythmic), Wyeth Recainam Tosylate (cardiac depressant; anti-arrhythmic), Wyeth Reclazepam (sedative), Searle Rimcazole HCI (antipsychotic), Burroughs Wellcome Salmeterol (bronchodilator), Glaxo Surfilcon A (contact lens material: hydrophilic), Permaflex, CooperVision Teicoplanin (antibacterial), Merrell Dow Temocillin (antibacterial), Beecham Tipentosin HCI (antihypertensive), Merrell Dow Tipredane (topical adrenocortical steroid), Squibb Tubulozole HCI (antineoplastic; microtubule inhibitor), Janssen Viprostol (hypotensive; vasodilator), Lederle Xylofilcon A (contact lens material: hydrophilic), Igel Optics, Ltd. Zaltidine HCI (histamine H[2] antagonist), Pfizer Zindotrine (bronchodilator), Merrell Dow