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TRPV1 Antagonist Pipeline<br />
81<br />
Compound<br />
AZD 1386<br />
MK 2295<br />
Merck/Neurogen<br />
Phase-II<br />
Pain<br />
JTS 653<br />
Japan Tobacco<br />
Phase-I<br />
Overactive bladder, Pain<br />
• Amgen stopped development of AMG-517 when patients<br />
Vanilloid receptor antagonists<br />
Renovis/Pfizer<br />
Phase-I<br />
Pain, Urinary incontinence<br />
experienced long-lasting hyper<strong>the</strong>rmia when treated with AMG-<br />
Asthma, Hypertension, Inflammation, Kidney disorders, Lung disorders,<br />
Ion channel modulators<br />
Hydra Biosciences Preclinical<br />
517 following molar extraction; some patients Osteoporosis, Overactive body bladder, temperature<br />
Pain<br />
Small molecule <strong>the</strong>rapeutics<br />
Amphora<br />
Preclinical CNS disorders, Metabolic disorders, Pain<br />
surpassed 40°C. It is possible that this problem i s due to off-<br />
Transient receptor potential vanilloid 1 cation<br />
Abbott Laboratories Preclinical Pain<br />
channel target antagonistseffects,<br />
as TRPV1 -/- mice do not exhibit hyper<strong>the</strong>rmia.<br />
TRPV • antagonists GSK’s SB-705498 Sanofi-Aventis showed promising Preclinical results Inflammation, Neuropathic in a study pain designed<br />
TRPV cation channel inhibitors<br />
Purdue Pharma<br />
Preclinical Pain<br />
to measure its ability to inhibit heat-evoked pain (capsaicin) and<br />
TRPV1 antagonists<br />
DiverDrugs<br />
Preclinical Inflammation, Pain<br />
skin sensitization (UV B irradiation). In addition, treatment with<br />
TRPV1 antagonists<br />
Eli Lilly<br />
Preclinical Inflammation, Pain, Urinary incontinence<br />
TRPV1 cation channel inhibitors<br />
Johnson & Johnson Preclinical Cough, Pain<br />
TRPV1 abandoned receptor antagonists development Traxion Therapeutics of <strong>the</strong> Preclinical drug, with Pain no explanation as to<br />
Vanilloid 1 receptor antagonists<br />
Vanilloid receptor antagonists<br />
Neurogen/Merck<br />
Preclinical Pain<br />
• In October 2008 Eli Lilly chose to suspend <strong>the</strong>ir trial for GRC-<br />
Vanilloid receptor antagonists<br />
Novartis<br />
Preclinical Neuropathic pain<br />
Vanilloid receptor antagonists<br />
TRPV1 cation channel inhibitors<br />
GRC 6211<br />
SB 705498<br />
AMG 517<br />
TRPV1 cation channel antagonists<br />
Developer<br />
AmorePacific/Schwarz<br />
Amgen<br />
Amgen<br />
Phase<br />
Preclinical<br />
Discontinued-II<br />
Discontinued-I<br />
Discontinued-<br />
Preclinical<br />
© Defined Health, 2009<br />
Pain Insight Briefing<br />
Indications<br />
Three TRPV1 antagonists AstraZeneca which Phase-II had entered Gastro-oesophageal <strong>the</strong> reflux, clinic Pain have been<br />
discontinued:<br />
400 mg of SB-705498 did not induce hyper<strong>the</strong>rmia. GSK has since<br />
why.<br />
6211, which <strong>the</strong>y were developing in collaboration with Glenmark,<br />
Pharmeste<br />
Preclinical Neuropathic pain, Urinary incontinence<br />
in OA. The companies Mochida Pharma/Wyeth have yet Research to publicly Pain disclose <strong>the</strong> reason<br />
<strong>the</strong> trial was ended Glenmark/Eli early. Lilly Discontinued-II Cystitis, Dental pain, Neuropathic pain, Urinary incontinence<br />
Adis R&D Insight; Nature Reviews Drug Discovery 8, 55-68 (January 2009)<br />
Pain
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