Safety and Efficacy of Asimadoline (TP0052) in Patients With Vasomotor Symptoms (VMS).

Not Applicable

Recruiting

• Conditions: Vasomotor Symptoms
• Interventions: Drug: Asimadoline

• Registration Number: NCT07042516
• Lead Sponsor: Tioga Pharmaceuticals

Brief Summary

This Randomized Clinical Trial entitled Safety and Efficacy of a Peripherally Restricted Selective Kappa Agonist for Moderate to Severe Menopausal Symptoms in Midlife Women is a Phase 2a randomized, double-blind, placebo-controlled trial evaluating the safety and efficacy of asimadoline TP0052 for the treatment of moderate to severe menopausal vasomotor symptoms (VMS). The design includes: 2 weeks of daily recording of VMS prior to drug treatment; 8 weeks of double-blind treatment with the peripherally restricted kappa agonist (PRKA), asimadoline TP0052, or placebo; and a safety telephone follow-up post-treatment; after the initial 8-week double-blinded follow-up, all patients undergo treatment with Asimadoline in an open label format for 4 weeks.

Detailed Description

Not available

Study Timeline

• Study First Submitted: 2025-06-19
• Study First Submitted QC: 2025-06-26
• Study First Posted: 2025-06-29
• Status Verified: 2025-07
• Study Start: 2025-07-01
• Last Update Submitted: 2025-07-01
• Last Update Posted: 2025-07-02
• Primary Completion: 2026-12-31
• Study Completion: 2027-02-20

Recruitment & Eligibility

• Status: RECRUITING
• Sex: Female
• Target Recruitment: 120

Inclusion Criteria

Not provided

Exclusion Criteria

• Known hypersensitivity to asimadoline TP0052.

• Chronic liver or renal disease, or uncontrolled seizure disorder.

• Use of medications or supplements that act as an inhibitor of P-glycoprotein or as a P-glycoprotein substrate during the 4 weeks prior to Screening Visit 1, including cyclosporine, non-topical ketoconazole, verapamil, digoxin, colchicine, sitagliptin).

• Blood test results indicating:

  • Liver function tests: AST ≥2 times upper limit of normal; ALT ≥2 times upper limit of normal; total bilirubin ≥ 1.5 times upper limit of normal
  • Kidney function test: estimated glomerular filtration rate (eGFR) < 60 mL/min/1.73 m²
  • Blood count: hematocrit <30%.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Asimadoline	Asimadoline	Asimadoline TP0052 2.5 mg two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily (10 mg) for 8 weeks. Post-unblinding 4 weeks of open label administration, TP0052 2.5 mg two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily (10 mg) for 4 weeks.
Placebo	Asimadoline	Placebo two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily for 8 weeks.
Asimadoline	Asimadoline	Asimadoline TP0052 2.5 mg two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily (10 mg) for 8 weeks. Post-unblinding 4 weeks of open label administration, TP0052 2.5 mg two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily (10 mg) for 4 weeks.
Placebo	Asimadoline	Placebo two (2) tablets bid (two on awakening and two before bed), total of four (4) tablets daily for 8 weeks.

Primary Outcome Measures

Name	Time	Method
Safety as Assessed by Adverse Events, Clinical Laboratory Parameters, and Vital Signs	baseline to 8 weeks	Safety will be evaluated based on the incidence and severity of adverse events and changes from baseline in laboratory values and vital signs. Adverse events will be graded using the Common Terminology Criteria for Adverse Events, Version 5.0 (grade 1 = mild; grade 5 = death; higher scores indicate worse outcomes). Liver function tests include alanine aminotransferase, aspartate aminotransferase, gamma-glutamyl transferase, alkaline phosphatase, and total bilirubin. Higher values indicate worse liver function. Kidney function will be assessed by estimated glomerular filtration rate (scale: 0 to ≥90 mL/min/1.73 m²; \<60 considered abnormal; higher is better). Hematocrit will be monitored (percent; \<30% is abnormal; higher is better within normal range). Vital signs include blood pressure, heart rate, respiratory rate, and oral temperature; higher blood pressure and heart rate indicate worse outcomes. A urine pregnancy test (positive or negative) will also be performed.

Secondary Outcome Measures

Name	Time	Method
Change in Frequency of Moderate to Severe Vasomotor Symptoms (VMS)	Baseline to 8 weeks	The frequency of moderate and severe vasomotor symptoms (VMS) will be measured using participant-completed diaries (paper or electronic) recorded twice daily (morning and evening) from Baseline to Week 8.; VMS frequency is defined as the number of moderate or severe hot flashes or night sweats reported per day.; Moderate VMS: sensation of heat with sweating, without disruption of activity. Severe VMS: sensation of heat with sweating that causes cessation of activity or awakening at night.; The outcome is calculated as the average number of moderate/severe VMS episodes per day, averaged over the 8-week treatment period.; Due to protocol-defined eligibility criteria, all participants will report at least 40 moderate/severe VMS episodes per week at baseline. During treatment, the minimum possible observed value is 0 episodes/day. There is no fixed upper limit; values of 20-30 episodes/day may occur.; Higher values indicate worse symptom frequency.
Change in Severity-Weighted Vasomotor Symptom (VMS) Score (Composite Severity Index).	Baseline to 8 weeks	VMS severity will be assessed using a composite score derived from participant diaries recorded twice daily from Baseline to Week 8.; Each VMS episode is assigned a severity score: Mild = 1 Moderate = 2 Severe = 3; Daily VMS severity scores are calculated as: (# Mild × 1) + (# Moderate × 2) + (# Severe × 3); Weekly averages of daily severity scores are computed for each participant. The average across the 8-week treatment period will serve as the outcome measure.; Due to protocol-defined eligibility criteria, all participants will report ≥40 moderate/severe VMS episodes per week at baseline. During treatment, the minimum possible observed value is 0. There is no fixed upper limit; for example, 10 severe episodes per day would result in a score of 30.; Higher scores indicate worse symptom severity.

Trial Locations

Locations (1)

Department of Gynecology & Obstetrics, Emory University School of Medicine; 🇺🇸 Atlanta, Georgia, United States