A Phase I Study to Investigate KH-001 in Healthy Males

NCT07868237 | Completed Phase 1 DMC FDA Drug

• 3 other identifiers: KH-001-01-012023-000058-832023
• Study Type: interventional
• Target: 82
• Locations: 1 country
• Sites: 1

Brief Summary

This was a Phase I, first-in-human study of KH-001 besylate in healthy male participants, conducted to investigate the safety, tolerability and pharmacokinetics (PK) of the study drug. The study was conducted in three parts: a single ascending dose (SAD) part, a multiple ascending dose (MAD) part, and a Formulation Effect part evaluating an orodispersible tablet (ODT) formulation. The study also evaluated the effect of KH-001 besylate on suicidality risk and mood. KH-001 besylate is being developed as an on-demand oral treatment for premature ejaculation.

Conditions

Healthy Male Volunteers

Keywords

KH-001; KH-001 besylate; premature ejaculation; first-in-human; single ascending dose; multiple ascending dose; pharmacokinetics; safety; tolerability; orodispersible tablet

Outcome Measures

Primary Outcomes (4)

• Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

  Number of participants with one or more treatment-emergent adverse events (TEAEs), including serious adverse events, summarized by severity and relationship to study drug. Adverse events were assessed by the investigator throughout the study.

  From first dose of study drug through the final follow-up visit (up to Day 12)

• Number of Participants With Clinically Significant Abnormal Clinical Laboratory Values

  Number of participants with clinically significant abnormal clinical laboratory results (clinical chemistry/biochemistry, hematology, coagulation and urinalysis), as determined by the investigator.

  From screening through the final follow-up visit (up to Day 12)

• Number of Participants With Clinically Significant Abnormal Vital Signs

  Number of participants with clinically significant abnormal vital sign findings (systolic and diastolic blood pressure, heart rate, respiratory rate and oral body temperature), as determined by the investigator.

  From screening through the final follow-up visit (up to Day 12)

• Number of Participants With Clinically Significant Abnormal 12-Lead ECG Findings

  Number of participants with clinically significant abnormal 12-lead electrocardiogram (ECG) findings (including heart rate and the RR, PR, QRS, QT and QTcF intervals), as determined by the investigator.

  From screening through the final follow-up visit (up to Day 12)

Secondary Outcomes (9)

• Maximum Plasma Concentration (Cmax) of KH-001

  Pre-dose to 24 hours post-dose (single dose; multiple-dose Days 1 and 5; each Formulation Effect period)

• Number of Participants With Suicidal Ideation or Behavior as Assessed by the Columbia-Suicide Severity Rating Scale (C-SSRS)

  From screening through the final follow-up visit (up to Day 12)

• In-Mouth Dissolution Time of the KH-001 Besylate Orodispersible Tablet (ODT)

  Formulation Effect dosing (Day 1 of each treatment period)

• Time to Maximum Plasma Concentration (Tmax) of KH-001

  Pre-dose to 24 hours post-dose (single dose; multiple-dose Days 1 and 5; each Formulation Effect period)

• Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUC0-t) of KH-001

  Pre-dose to 24 hours post-dose (single dose; each Formulation Effect period)

Study Arms (3)

KH-001 besylate (SAD and MAD)

EXPERIMENTAL

Single (7 doses) or multiple ascending (2 doses) doses of KH-001 besylate oral solution

Drug: KH-001 besylate

Placebo (SAD and MAD)

PLACEBO COMPARATOR

Matching placebo administered by oral solution

Drug: KH-001 besylate placebo

KH-001 besylate ODT (Formulation Effect)

EXPERIMENTAL

KH-001 besylate orodispersible tablet at two dose strengths, fixed-sequence crossover

Drug: KH-001 besylate

Interventions

KH-001 besylate DRUG

Associated arm(s): 1 and 3

KH-001 besylate (SAD and MAD); KH-001 besylate ODT (Formulation Effect)

KH-001 besylate placebo DRUG

Associated arm(s): Arm 2 (Placebo)

Placebo (SAD and MAD)

Eligibility Criteria

• Age: 18 Years - 64 Years
• Gender Eligibility Details: Study recruited cisgender males only
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy male between 18 and 64 years of age, inclusive.
• For male participants with a female partner of childbearing potential, the contraception requirements for participation required the use of a condom by the male in addition to either one other highly effective method of contraception, or one other effective method of contraception by the female partner, if applicable, from first dose until 3 months after last dose.
• Body mass index (BMI) of 18-30 kg/m2.
• No clinically significant history of previous allergy / sensitivity to the investigational medicinal product (IMP) or any of the excipients contained within the IMP(s).
• No clinically significant abnormal test results for serum biochemistry, hematology and/or urine analyses within 28 days before the first dose administration of the IMP.
• Negative urinary drugs of abuse (DOA) screen (including alcohol) test results, determined within 28 days before the first dose administration of the IMP.
• Negative human immunodeficiency virus (HIV), hepatitis B surface antigen (HBsAg) and hepatitis C virus antibody (HCV Ab) test results at Screening.
• No clinically significant abnormalities in 12-lead electrocardiogram (ECG) determined within 28 days before first dose of IMP including a PR interval \> 220 ms, QT interval corrected using Fridericia's formula QTcF \> 450 ms.
• No clinically significant abnormalities in vital signs (blood pressure/heart rate, respiratory rate, oral temperature) determined within 28 days before first dose of IMP.
• Available to complete the study (including all follow-up visits).
• Satisfied an Investigator about participant fitness to participate in the study.
• Provided written informed consent to participate in the study.

You may not qualify if:

• A clinically significant history of gastrointestinal disorder likely to influence IMP absorption.
• Allergic reaction to the IMP or history of reaction to relevant supplements.
• Use of prescription or non-prescription drugs, including vitamins, herbal and dietary supplements within 28 days or 5 half-lives (whichever is longer) prior to the first dose of IMP.
• Evidence of any clinically significant history or the presence of renal, hepatic, respiratory, cardiovascular (hypertension, unstable angina, arrhythmia, QT prolongation, etc.), metabolic dysfunction, hematological, lymphatic or neurological diseases.
• Disorders of the central nervous system, psychiatric disorders, behavioral/behavior disturbances (e.g., cerebrovascular events, depression, post-traumatic stress disorder \[PTSD\], anxiety, bipolar disorder, severe migraine, Parkinson's disease).
• History of narrow angle glaucoma.
• Have had a tattoo or piercing in the 3 months prior to Screening.
• Reported having experienced suicidal ideation (Type 4 or 5 on the Columbia-Suicide Severity Rating Scale \[C-SSRS\]) within 28 days prior to Screening, any suicidal behavior within 2 years prior to Screening (any "Yes" answers on the Suicidal Behavior section of C-SSRS), and/or the Investigator assessed the participant to be a safety risk to himself/herself or others.
• Past history of prostate cancer, benign prostatic hyperplasia (BPH) or other clinically significant prostate disease.
• Concomitant disease or condition that could have interfered with, or treatment which may have interfered with, the conduct of the study, or that would, in the opinion of the investigator, have posed an unacceptable risk to the participant in this study.
• Concomitant use of CNS medications (including anti-depressants, anti-psychotics), tramadol, topical anesthetics, phosphodiesterase 5 (PDE5) inhibitors or vasoactive penile injection therapy.
• A clinically significant current or history of drug or alcohol abuse (defined as the consumption of more than 14 units \[for male participants\] of alcohol a week) within the past two years.
• Inability to communicate well with the Investigators (i.e., language problem, poor mental development or impaired cerebral function).
• Participation in a New Chemical Entity (NCE) clinical study within the previous 3 months or five half-lives, whichever is longer, or a marketed drug clinical study within the 30 days or five half-lives, whichever is longer, before the first dose of IMP. (Washout period between studies is defined as the period of time elapsed between the last dose of the previous study and the first dose of the next study.)
• Donation of 450 mL or more blood within the 3 months before the first dose of IMP.

Sponsors & Collaborators

• Kadence Bio: lead

Study Sites (1)

Simbec-Orion Clinical Pharmacology Unit

Merthyr Tydfil, South Wales, CF48 4DR, United Kingdom

Location

MeSH Terms

Conditions

Premature Ejaculation

Condition Hierarchy (Ancestors)

Ejaculatory Dysfunction; Genital Diseases, Male; Genital Diseases; Urogenital Diseases; Sexual Dysfunction, Physiological; Male Urogenital Diseases; Sexual Dysfunctions, Psychological; Mental Disorders

Study Officials

• Annelize Koch, Dr

  Simbec-Orion Ltd

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Masking Details: Double-blind
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Model Details: The study comprised three parts. SAD: 56 participants across 7 sequential dose-escalation cohorts of 8 (randomized 3:1 to KH-001 besylate or placebo), single dose. MAD: 18 participants across 2 sequential cohorts of 9 (randomized 2:1), once daily for 5 days. Formulation Effect: 8 participants in a non-randomized, open-label, fixed-sequence crossover comparing the oral solution with an ODT at two dose strengths.

Study Record Dates

• First Submitted: September 25, 2026
• First Posted: October 9, 2026
• Study Start: November 14, 2023
• Primary Completion: August 28, 2025
• Study Completion: August 28, 2025
• Last Updated: October 9, 2026

Record last verified: 2026-10

Data Sharing

• IPD Sharing: Will not share

Locations

GB (1)