Lotilaner

Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites. Inhibition of these GABA chloride channels causes a paralytic action in the target organism leading to its death.

• XDEMVY is indicated for the treatment of Demodex blepharitis. XDEMVY is an ectoparasiticide (anti-parasitic) indicated for the treatment of Demodex blepharitis.

• None. None.contraindicated

Instill one drop of XDEMVY in each eye twice daily (approximately 12 hours apart) for 6 weeks. If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart. If one dose is missed, treatment should continue with the next scheduled dose. Instill one drop of XDEMVY in each eye twice daily (approximately 12 hours apart) for 6 weeks. ( 2 )

5.1 Risk of Contamination Do not allow the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to minimize contamination of the solution. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions . 5.2 Use with Contact Lenses Contact lenses should be removed prior to instillation of XDEMVY and may be reinserted 15 minutes following its administration.

The most common adverse reaction was instillation site stinging and burning (10%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Tarsus Pharmaceuticals at 1-888-421-4002 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical studies 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. XDEMVY was evaluated in 833 patients with Demodex blepharitis in two randomized, double-masked, vehicle-controlled studies (Saturn-1 and Saturn-2) with 42 days of treatment. The most common ocular adverse reaction observed in controlled clinical studies with XDEMVY was instillation site stinging and burning which was reported in 10% of patients. Other ocular adverse reactions reported in less than 2% of patients were chalazion/hordeolum and punctate keratitis.

8.1 Pregnancy Risk Summary There are no available data on XDEMVY use in pregnant women to inform any drug associated risk; however, systemic exposure to lotilaner from ocular administration is low [see Clinical Pharmacology (12.3) ] . In animal reproduction studies, lotilaner did not produce malformations at clinically relevant doses. Data Animal Data In an oral embryofetal developmental study in pregnant rats dosed during organogenesis from gestation days 6-19, increased post-implantation loss, reduced fetal pup weight, and incomplete skeletal ossification were observed at 50 mg/kg/day (approximately 1390 times the recommended human ophthalmic dose (RHOD) on a body surface area basis) in the presence of maternal toxicity (i.e., decreased body weight and food consumption). A rare malformation of situs inversus of the thoracic and abdominal viscera occurred in 1 fetus from a pregnant rat receiving 50 mg/kg/day; whether this finding was treatment-related could not be excluded. No maternal or embryofetal toxicity was observed at 18 mg/kg/day (approximately 501 times the RHOD on a body surface area basis).

Metabolism

The systemic pharmacokinetic profile after topical ocular administration was evaluated in healthy volunteers after single and repeat dose administration. The systemic exposure was evaluated in patients at the end of 6 weeks of treatment.

• Jul 24, 2023NDANDA217603Tarsus

1. 1Eye Irritation33013%
2. 2Ocular Hyperaemia2208.8%
3. 3Vision Blurred2068.2%
4. 4Eye Pain1917.6%
5. 5Off Label Use1837.3%
6. 6Product Use Issue1837.3%
7. 7Condition Aggravated1736.9%
8. 8Wrong Technique In Product Usage Process1465.8%
9. 9Therapy Interrupted1445.8%
10. 10Eye Pruritus1385.5%
11. 11Instillation Site Irritation1094.4%
12. 12Lacrimation Increased1044.2%
13. 13Drug Ineffective1034.1%
14. 14Eye Swelling903.6%
15. 15Headache873.5%

The 10 most recently updated of 13 ClinicalTrials.gov registrations naming Lotilaner as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study to Evaluate Safety and Efficacy of TP-05 in Healthy Participants With Tick Exposure
  Recruiting · Phase 2 · Interventional · 700 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT07562087updated 2026-05-20
• Study of Lotilaner Ophthalmic Gel in Patients With Ocular Rosacea (KORE)
  Enrolling by invitation · Phase 2 · Interventional · 155 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT07443202updated 2026-03-02
• Pilot Study Comparing the Safety and Efficacy of Two Dosing Regimens of TP-03 for the Treatment of MGD
  Completed · Phase 2 · Interventional · 39 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT05454956updated 2025-10-01
• Impact of XDEMVY® on Demodex Blepharitis in Soft Contact Lens Wearers
  Completed · Phase 4 · Interventional · 145 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT06182358updated 2025-07-02
• A Human Tick Kill Study to Investigate the Safety, Tolerability, and Whole Blood Concentration of TP-05
  Completed · Phase 2 · Interventional · 30 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT05387083updated 2024-09-19
• Trial to Evaluate the Efficacy and Safety of TP-03, LIBRA Study
  Completed · Phase 3 · Interventional · 163 enrolled · LianBio LLC
  NCT05629390updated 2024-05-21
• A Six Week Pharmacokinetic Study of TP-03 in Healthy Subjects
  Completed · Phase 1 · Interventional · 24 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT05138861updated 2024-04-12
• Effect of an Exploratory Vehicle on Meibomian Gland Dysfunction in Patients With Demodex
  Unknown · Phase 2 · Interventional · 36 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT06054217updated 2024-04-09
• Trial to Evaluate the Safety and Efficacy of TP-03 for the Treatment of Demodex Blepharitis
  Completed · Phase 3 · Interventional · 412 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT04784091updated 2023-12-21
• Safety and Efficacy of TP-03 for the Treatment of Demodex Blepharitis
  Completed · Phase 2 · Phase 3 · Interventional · 421 enrolled · Tarsus Pharmaceuticals, Inc.
  NCT04475432updated 2023-12-21

Frequently asked questions

How does Lotilaner work?

Lotilaner is a gamma-aminobutyric acid (GABA)-gated chloride channel inhibitor selective for mites. Inhibition of these GABA chloride channels causes a paralytic action in the target organism leading to its death.

What is Lotilaner used for?

According to FDA labeling, Lotilaner carries indications including: XDEMVY is indicated for the treatment of Demodex blepharitis. XDEMVY is an ectoparasiticide (anti-parasitic) indicated for the treatment of Demodex blepharitis.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Lotilaner?

Lotilaner is classified as Other antiinfectives, Ectoparasiticide.

What are the brand names for Lotilaner?

Lotilaner is marketed under brand names including Credelio, Xdemvy.

What are the contraindications for Lotilaner?

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