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 molecular structure | |
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| Trade names | Tryptyr |
| Other names | AVX-012, WS-12 |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a625071 |
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| Routes of administration | Eye drop |
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| DrugBank | |
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| CompTox Dashboard (EPA) | |
| Chemical and physical data | |
| Formula | C18H27NO2 |
| Molar mass | 289.419 g·mol−1 |
| 3D model (JSmol) | |
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Acoltremon sold under the brand name Tryptyr, is a medication used for the treatment of dry eye syndrome.[1] Acoltremon is a transient receptor potential melastatin 8 (TRPM8) thermoreceptor agonist.[1] It is used as an eye drop.[1]
The most common treatment-emergent adverse event experienced during the clinical studies was instillation site pain (burning or stinging) events.[2]
Acoltremon was approved for medical use in the United States in May 2025.[2]
Acoltremon is indicated for the treatment of the signs and symptoms of dry eye disease.[1][2]
Acoltremon acts as a potent and selective activator (opener) of the TRPM8 calcium channel, which is responsible for the sensation of coldness produced by menthol.[3] It is slightly less potent as a TRPM8 activator compared to icilin, but is a much more selective TRPM8 ligand when compared to menthol.[4]
The US Food and Drug Administration (FDA) approved acoltremon based on evidence from two clinical trials (COMET-2 and COMET-3) of 931 participants with dry eye disease.[2] The trials were conducted at 46 sites in the United States.[2] Two additional studies: COMET-1 and COMET-4 were included in the evaluation of safety benefit of acoltremon.[2] The number of participants representing efficacy findings may differ from the number of participants representing safety findings due to different pools of study participants analyzed for efficacy and safety.[2] Both COMET-2 and COMET-3 are phase III, multi-center, vehicle-controlled, double-masked, randomized studies whose primary endpoint was proportion of participants with ≥10 mm increase from baseline in unanesthetized Schirmer Score on day 14.[2] COMET-1 was a phase IIb multi-center, vehicle-controlled, double-masked, randomized study conducted at 15 sites in the United States which randomized 369 participants with a history of dry eye disease.[2] COMET-4 was a multi-center, vehicle-controlled, double-masked, randomized study conducted at approximately 10 sites in the United States which enrolled 275 participants with a history of dry eye disease.[2] Study COMET-2 and COMET-3 have a similar design.[2] Each study is a multi-center, randomized, double-masked, vehicle-controlled phase III study.[2] The primary objective of these studies was to evaluate the safety and efficacy of acoltremon compared to vehicle.[2] Participants 30 years and older with a history of artificial tear use for dry eye disease were qualified based on signs and symptoms of dry eye disease at screening, and were requalified at baseline (day 1) following a 14-day vehicle run-in.[2] COMET 2 enrolled 465 participants at 23 study sites, whereas COMET-3 enrolled 466 participants at 23 sites.[2]
Acoltremon was approved for medical use in the United States in May 2025.[5]
Acoltremon is the international nonproprietary name.[6]
Acoltremon is sold under the brand name Tryptyr.[2]
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