Acoltremon

Studies in animals suggest that acoltremon, the active substance in TRYPTYR, is an agonist of transient receptor potential melastatin 8 (TRPM8) thermoreceptors. TRPM8 thermoreceptor stimulation has been shown to activate trigeminal nerve signaling leading to increased basal tear production.

• TRYPTYR is indicated for the treatment of the signs and symptoms of dry eye disease. TRYPTYR is a TRPM8 thermoreceptor agonist indicated for the treatment of the signs and symptoms of dry eye disease.

• None. None.contraindicated

Instill one drop in each eye twice daily (approximately 12 hours apart). ( 2 ) 2.1 Recommended Dosage Instill one drop in each eye twice daily (approximately 12 hours apart). 2.2 Administration Instructions Wash hands before use. The single-dose vials are to be used immediately after opening and can be used to dose both eyes. Discard the single-dose vial, including any remaining contents, immediately after use. TRYPTYR can be used concomitantly with other topical ophthalmic eye drops. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart . Contact lenses should be removed prior to the administration of TRYPTYR and may be reinserted 15 minutes following administration. If one dose is missed, treatment should continue with the next dose.

To avoid the potential for eye injury and contamination, do not touch the vial tip to the eye or other surfaces. ( 5.1 ) 5.1 Potential for Eye Injury and Contamination To avoid the potential for eye injury and contamination, do not touch the vial tip to the eye or other surfaces. 5.2 Use with Contact Lenses TRYPTYR should not be administered while wearing contact lenses. If contact lenses are worn, they should be removed prior to administration of the solution. Lenses may be reinserted 15 minutes following administration of TRYPTYR.

The most common adverse reaction was instillation site pain (50%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Alcon Laboratories, Inc. at 1-800-757-9780, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In patients with dry eye disease, 766 patients received at least one dose of TRYPTYR in four randomized controlled clinical trials across 71 sites in the United States. The most common ocular adverse reaction observed in controlled clinical studies with TRYPTYR was instillation site pain (50%). Less than 1% of patients discontinued therapy due to burning or stinging sensation in the eyes.

8.1 Pregnancy Risk Summary There are no adequate and well-controlled studies on TRYPTYR in pregnant women. Systemic exposure to acoltremon from ocular administration is negligible [see Clinical Pharmacology ( 12.3 )] . Intravenous administration of acoltremon to pregnant rats and rabbits during organogenesis did not produce embryofetal toxicity at 806- and 2151-fold the maximum recommended human ocular dose (MRHOD) of acoltremon on a mg/m 2 basis ( see Data ) . All pregnancies have a risk of birth defect, loss, or other adverse outcomes. In the US general population, the estimated background risk of major birth defects is 2 to 4%, and of miscarriage is 15 to 20%, of clinically recognized pregnancies. Data Animal Data In embryofetal developmental studies in pregnant rats and rabbits dosed by intravenous injection daily during organogenesis from gestation days 6-17 and gestation days 7-19, respectively, no maternal or fetal toxicity was observed at 806- and 2151-fold the MRHOD of acoltremon on a mg/m 2 basis. 8.2 Lactation Risk Summary There are no data on the presence of acoltremon in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to acoltremon following topical ocular administration is low.

Metabolism

PK was assessed in 25 patients with dry eye disease receiving TRYPTYR administration (1 drop twice daily) on Days 1, 14, and 90. A total of three (3) (12.0%) had plasma concentrations above 20 pg/mL (the lower limit of quantification), with the highest plasma concentration of 213 pg/mL.

• May 28, 2025NDANDA217370Alcon Labs Inc

1. 1Eye Irritation1,46254%
2. 2Eye Pain48818%
3. 3Drug Ineffective48018%
4. 4Ocular Hyperaemia2328.6%
5. 5Vision Blurred2228.2%
6. 6Condition Aggravated1465.4%
7. 7Lacrimation Increased1254.6%
8. 8Ocular Discomfort1164.3%
9. 9Dry Eye1144.2%
10. 10Eye Pruritus983.6%
11. 11Headache833.1%
12. 12Eye Swelling501.9%
13. 13Visual Impairment491.8%
14. 14Dizziness451.7%
15. 15Drug Hypersensitivity451.7%

The 10 most recently updated of 10 ClinicalTrials.gov registrations naming Acoltremon as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Effect of Acoltremon Ophthalmic Solution 0.003% on Signs and Symptoms of Ocular Surface Disease in Stage I Neurotrophic Keratopathy Patients With Tear Deficiency
  Recruiting · Phase 4 · Interventional · 50 enrolled · University of South Florida
  NCT07502378updated 2026-03-31
• A Study to Investigate the Effect of 0.003% AR-15512 on Subjects With Dry Eye Disease
  Completed · Phase 3 · Interventional · 80 enrolled · Alcon Research
  NCT06544694updated 2026-03-27
• A Study to Evaluate 0.003% AR-15512 Safety and Drop Attributes
  Completed · Phase 3 · Interventional · 55 enrolled · Alcon Research
  NCT06660290updated 2026-03-17
• A Study Designed to Evaluate Tear Production
  Completed · Phase 3 · Interventional · 81 enrolled · Alcon Research
  NCT06544707updated 2026-02-10
• Evaluating a New Therapy for Dry Eye in Patients With Sjögren's Syndrome
  Recruiting · Phase 4 · Interventional · 35 enrolled · Center For Sight
  NCT07277257updated 2025-12-22
• Investigator Initiated Trial Using Dry Eye Surveys to Evaluate and Better Understand FDA Approved Acoltremon Treatment for Dry Eye Disease in Real World Treatment Settings (DESERT)
  Not yet recruiting · Phase 4 · Interventional · 60 enrolled · Center for Sight Las Vegas
  NCT07281950updated 2025-12-17
• Moderate-to-Severe Dry Eye Disease Relief Using Acoltremon
  Enrolling by invitation · Observational · 50 enrolled · Colvard Kandavel Eye Center
  NCT07268599updated 2025-12-08
• Switching From Restasis to TRYPTYR
  Not yet recruiting · Phase 4 · Interventional · 100 enrolled · Southern College of Optometry
  NCT07267299updated 2025-12-05
• Impact of TRYPTYR on a Patient's Quality of Life and Ability to Perform Work
  Recruiting · Phase 4 · Interventional · 40 enrolled · Southern College of Optometry
  NCT07266948updated 2025-12-05
• Switching From Xiidra to TRYPTYR
  Not yet recruiting · Phase 4 · Interventional · 100 enrolled · Southern College of Optometry
  NCT07267481updated 2025-12-05

Frequently asked questions

How does Acoltremon work?

Studies in animals suggest that acoltremon, the active substance in TRYPTYR, is an agonist of transient receptor potential melastatin 8 (TRPM8) thermoreceptors. TRPM8 thermoreceptor stimulation has been shown to activate trigeminal nerve signaling leading to increased basal tear production.

What is Acoltremon used for?

According to FDA labeling, Acoltremon carries indications including: TRYPTYR is indicated for the treatment of the signs and symptoms of dry eye disease. TRYPTYR is a TRPM8 thermoreceptor agonist indicated for the treatment of the signs and symptoms of dry eye disease.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Acoltremon?

Acoltremon is classified as TRPM8 Thermoreceptor Agonist, Ion Channel Interactions, TRPM8 Thermoreceptor Agonists.

What are the brand names for Acoltremon?

Acoltremon is marketed under brand names including Tryptyr.

What are the contraindications for Acoltremon?

Acoltremon labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.