Enter drug's generic or brand name below. Results will appear here. Note: all drug related information obtained on this page is provided by RX List.
Using the RX LIST database:
(1) Enter the drug name in the search box below and hit ENTER
(2) The rx list web site will open here with the drug search completed. Next, scroll down the page to locate the link to the drug you are searching for and then click on the link.
TRYPTYR (acoltremon ophthalmic solution) 0.003% contains an agonist of TRPM8 ion channels. Acoltremon’s chemical name is (1R,2S,5R)-2-isopropyl-N-(4-methoxyphenyl)-5-methylcyclohexane-1carboxamide. The molecular formula of acoltremon is C18H27NO2 and has a molecular weight of 289.42 g/mol.
 |
Acoltremon is a white to pale yellow crystalline solid, that is insoluble in water.
TRYPTYR is a sterile, clear to slightly opalescent, colorless, isotonic aqueous solution for topical ophthalmic use, with a pH of approximately 7 and an osmolality of 280 to 330 mOsm/kg. Each mL of TRYPTYR contains active: acoltremon 0.003%; and inactives: polyoxyl 35 castor oil, sodium dihydrogen phosphate dihydrate, sodium chloride, hypromellose and purified water. Additionally, sodium hydroxide is used to adjust pH. TRYPTYR does not contain an anti-microbial preservative.
TRYPTYR is indicated for the treatment of the signs and symptoms of dry eye disease.
Instill one drop in each eye twice daily (approximately 12 hours apart).
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.
TRYPTYR is a clear to slightly opalescent, colorless ophthalmic solution containing 0.003% acoltremon in a single-dose vial.
TRYPTYR (acoltremon ophthalmic solution) 0.003% is supplied as a sterile, clear to slightly opalescent, and colorless solution in a low-density polyethylene (LDPE), single-dose vial with a 0.4 mL fill. One strip of 5 single-dose vials is packaged in a foil pouch with twelve (12) pouches in a carton.
NDC 00658-595-02; Carton of 60 Single-Dose Vials.
Store refrigerated at 2°C to 8°C (36°F to 46°F). After opening the carton, TRYPTYR may be stored refrigerated or at room temperature at 2°C to 25°C (36°F to 77°F). If stored at room temperature, TRYPTYR should be used within 30 days, not to exceed the expiration date printed on the carton and foil pouch.
After opening each foil pouch, the single-dose vials should be used within 7 days, not to exceed the expiration date printed on the vial. Store unopened single-dose vials in the original foil pouch until ready to use.
Manufactured for: Alcon Laboratories, Inc. Fort Worth, TX 76134, U.S.A. Revised: May 2025
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.
No Information Provided
Included as part of the "PRECAUTIONS" Section
To avoid the potential for eye injury and contamination, do not touch the vial tip to the eye or other surfaces.
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.
Advise patients to read the FDA-approved patient labeling (Instructions for Use).
Advise patients not to touch the tip of the single-dose vial to their eye or to any surface in order to avoid eye injury or contamination of the solution [see WARNINGS AND PRECAUTIONS].
Advise patients that one single-dose vial can be used to dose both eyes immediately after opening. Discard the single-dose vial, including any remaining contents, after use [see DOSAGE AND ADMINISTRATION].
Advise patients that contact lenses should be removed prior to administration of TRYPTYR and can be reinserted 15 minutes after administration [see WARNINGS AND PRECAUTIONS].
Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart [see DOSAGE AND ADMINISTRATION].
Instruct patients to store unopened single-dose vials in the original foil pouch until ready to use [see HOW SUPPLIED].
Long term studies in animals have not been performed to evaluate the carcinogenic potential of acoltremon.
Acoltremon was not mutagenic or clastogenic in the standard battery of genotoxicity tests including a bacterial reverse mutation assay, an in vitro chromosomal aberration assay in human peripheral lymphocytes and micronucleus assay in rats.
Studies to evaluate the potential effects of acoltremon on male or female fertility in animals have not been performed.
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 ]. 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/m2 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.
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/m2 basis.
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. The lack of clinical data during lactation precludes a clear determination of the risk of TRYPTYR to an infant during lactation; however, the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for TRYPTYR.
The safety and effectiveness of TRYPTYR have not been established in pediatric patients.
No clinically relevant differences in safety have been observed between elderly and younger patients.
No Information Provided
None.
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. The exact mechanism of action for TRYPTYR in dry eye disease is unknown.
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.
The efficacy of TRYPTYR for the treatment of dry eye disease was supported by two randomized, multi-center, double-masked, vehicle-controlled studies (COMET-2 [NCT-05285644] and COMET-3 [NCT-05360966]) enrolling a total of 931 dry eye patients (462 of which received TRYPTYR). Patients were randomized to TRYPTYR or vehicle (placebo) in a 1:1 ratio and dosed twice a day for 90 days. Use of artificial tears was not allowed during the studies. The mean age was 61 years (range, 30-93 years). The majority of patients were female (74.8%). Enrollment criteria included signs (i.e., corneal fluorescein staining score [2-15] and anesthetized Schirmer tear test [2-9 mm]) and symptoms (i.e., SANDE Score [≥ 50] and Ocular Discomfort Score [≥ 50]) of dry eye disease.
Tear film production was measured by unanesthetized Schirmer tear test assessed using a Schirmer strip (0 - 35 mm). The average baseline unanesthetized Schirmer scores for TRYPTYR and Vehicle treated patients was 6.2 mm and 5.9 mm in the COMET-2 study, and 6.8 mm and 6.4 mm in the COMET-3 study, respectively. Of the patients treated at Day 14 (primary endpoint) with TRYPTYR, 42.6% achieved ≥ 10 mm increase in Schirmer score from baseline in the COMET-2 study and 53.2% achieved ≥ 10 mm increase in Schirmer score from baseline at Day 14 in the COMET-3 study, compared to 8.2% and 14.4% of vehicle-treated patients in the COMET-2 study and the COMET-3 study, respectively. A statistically significant improvement in tear production favoring TRYPTYR (p<0.01) was observed in both studies (Table 1).
Table 1: Percent of Patients Achieving ≥ 10 mm Improvement from Baseline in Schirmer Score at Day 14 in Patients with Dry Eye Disease
| Tear Production | ||||
| COMET-2 | COMET-3 | |||
| TRYPTYR N = 230 |
Vehicle N = 235 |
TRYPTYR N = 232 |
Vehicle N = 234 |
|
| ≥ 10 mm increase in tear production at Day 14 | 42.6% | 8.2% | 53.2% | 14.4% |
| Difference (95% CI) | 34.4% (26.9, 42.0) | 38.8% (30.8, 46.8) | ||
| P-value versus vehicle | < 0.01 | < 0.01 | ||
Consistent results were observed at all timepoints through Day 90.
INSTRUCTIONS FOR USE
TRYPTYR®
[trip’tir]
(acoltremon ophthalmic solution) 0.003% for topical ophthalmic use
This Instructions for Use contains information on how to use TRYPTYR. Read this Instructions for Use before you start using TRYPTYR and each time you get a refill. There may be new information. This leaflet does not take the place of talking to your healthcare provider about your medical condition or your treatment.
 |
 |
 |
Important Information You Need to Know Before Using TRYPTYR:
Follow steps 1 to 15 each time you use TRYPTYR
Step 1
 |
Step 2
Preparing a single-dose vial
Step 3
 |
Step 4
 |
Step 5
 |
Step 6
 |
Step 7
 |
Applying a dose of TRYPTYR to your eyes
Step 8
Step 9
Step 10
Step 11
 |
Step 12
After dosing and disposal instructions
Step 13
 |
Step 14
 |
Step 15
 |
How should I store TRYPTYR?
This Instructions for Use has been approved by the U.S. Food and Drug Administration.
