GLAXO PLANS TO FOLLOW UP ZANTAC WITH LONG-ACTING SUFOTIDINE; H[2] ANTAGONIST IS ONE OF SEVEN DRUGS TARGETED FOR WORLDWIDE MARKETING APPLICATIONS IN 1988-90

Glaxo is developing the long-acting H[2] antagonist sufotidine as a follow-up compound to Zantac (ranitidine), the company indicated in its just-released annual report for the fiscal year ended June 30, 1987. "Extensive clinical trials are imminent on sufotidine, which is a competitive histamine H[2] antagonist like ranitidine, but is longer acting because of its slower absorption and excretion," the annual report states. Glaxo identified one objective of its gastrointestinal R&D program as improving the management of reflux esophagitis. Meanwhile, Zantac continues to show solid growth in the worldwide anti-ulcer market, where sales increased 37% to about $1.3 bil. in fiscal 1987. [EDITORS' NOTE: Glaxo's annual report provides results in pounds. Currency translation is at one British Pound = 1.62 U.S. dollars, the June 30 exchange rate.] Roughly half of that volume occurred in the U.S. -- Zantac sales were up 44% to $656 mil., making up 70% of Glaxo's $937 mil. U.S. drug business. By the end of the fiscal year, Zantac had improved its share of the U.S. anti-ulcer market to 44%, up seven share points from fiscal 1986, the report notes. Zantac's U.S. patent expires in 1993. Sufotidine is one of at least seven drugs in four therapeutic groups that Glaxo is targeting for regulatory submissions in various countries between 1988 and 1990. The central nervous system agent GR 38032 is in clinicals as an anti-emetic in conjuction with chemotherapy and is under investigation for use in treating anxiety and schizophrenia. A second compound, GR 43175, is in trials for the prevention and treatment of migraine. Both compounds involve 5-hydroxytryptamine receptors -- GH 38032 acts as an antagonist, GR 43175 as an agonist. Two cardiovascular compounds have also reached clinicals. GR 32191, an oral thromboxane A[2] antagonist "is being studied clinically in occlusive vascular diseases and may be of special value for treating atheromatous disease and its complications," the annual report notes. The drug inhibits aggregation of blood platelets and can potentially inhibit thrombus formation in blood vessels. Lacidipine (GR 43659), a calcium channel blocker, is under development as a once-daily treatment for hypertension. Salmeterol, a long-acting beta-stimulant bronchodilator, is one of two respiratory agents in full-scale clinical development for treatment of asthma. The other, fluticasone, is an anti-inflammatory steroid. Like salmeterol, fluticasone is administered by inhalation. In addition to the currently marketed bronchodilator Ventolin (albuterol), the company has an NDA pending in the U.S. for an oral, controlled-release formulation developed by Alza. Glaxo's corporate fiscal 1987 volume grew 27% to $2.8 bil., the company reported. Nearly half of the company's sales, or about $1.35 bil., came from Zantac. Of Glaxo's total volume, only about 13%, or $369 mil., occurred in the U.K., where the company is based. Sales of Glaxo Inc., the firm's U.S. subsidiary, grew 51% in fiscal 1987 to $937 mil. Following Zantac in fiscal 1987, worldwide sales by therapeutic category were respiratory products ($586 mil.), systemic antibiotics ($366 mil.), and dermatologicals ($139 mil.). The company said the growth rate achieved in sales of cephalosporins, which "far exceeded the growth in the world market," was attributable to the performance of the injectable product Fortaz (ceftazidime). Ceftazidime worldwide sales grew 49% in fiscal 1987 to $188 mil. "At the same time Glaxo increased the level of sales of its earlier injectable cephalosporin, Zinacef (cefuroxime) and of the oral antibiotic Ceporex (cephalexin)," the annual report states.