CAS NO 334476-46-9
Elemental Analysis: C, 56.21; H, 4.92; F, 27.06; N, 8.55; O, 3.26
Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression.
Vestipitant is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitus.
Vestipitant mesylate is a tachykinin NK1 receptor antagonist in phase II clinical trials at GlaxoSmithKline for the treatment of postoperative nausea and vomiting. The drug candidate had been in clinical development at the company for several indications, including the treatment of tinnitus as monotherapy or in combination with paroxetine, the treatment of primary insomnia, the treatment of depression and anxiety and the treatment of chemotherapy-induced nausea and vomiting; however, no recent development has been reported for this research.
Vestipitant has anxiolytic properties and a good safety profile. Vestipitant was investigated for potential effect against chronic tinnitus as a stand-alone treatment and in conjunction with a selective serotonin reuptake inhibitor, paroxetine. No statistically significant treatment benefit effect was detected for tinnitus (intensity, pitch, and distress) VAS scores, arousal-anxiety VAS scores, Tinnitus Handicap Inventory, or tinnitus aggravation scores assessed on Days 1 and 14. However, a statistically significant worsening of tinnitus intensity and distress scores was observed after vestipitant compared with placebo for the mean data collected over the treatment period. No relevant differences in vestipitant plasma concentrations were observed between the subjects given the combination with paroxetine and those receiving vestipitant alone. No specific relationships were observed between tinnitus intensity and vestipitant plasma concentrations.
CONCLUSION: Although well-tolerated vestipitant, alone or in combination with paroxetine, was not effective in ameliorating tinnitus in this patient group.
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- ClinicalTrials.gov NCT00394056 Vestipitant Or Vestipitant/Paroxetine Combination In Subjects With Tinnitus And Hearing Loss
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DR ANTHONY MELVIN CRASTO Ph.D
GLENMARK SCIENTIST , NAVIMUMBAI, INDIA
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