A First-in-Human SAD and MAD Study in Healthy Participants to Evaluate Oral YR011 Tablet

NCT07285967 | Not Yet Recruiting Phase 1 FDA Drug

• 1 other identifier: YR011-B01
• Study Type: interventional
• Target: 64
• Locations: 0 countries
• Sites: N/A

Brief Summary

This is a Phase I clinical trial (protocol number: YR-011-B01) sponsored by Hangzhou Yirui Pharmaceutical Technology Co., Ltd., focusing on the novel oral small-molecule drug YR011 (active ingredient: PA032, a Kv1.3 channel blocker). The trial aims to evaluate the safety, tolerability, and pharmacokinetics (PK) of YR011 in healthy adult participants. The trial has two stages: Single Ascending Dose (SAD) and Multiple Ascending Dose (MAD), with about 64 participants total (32 per stage). Participants are divided into 4 cohorts per stage (8 people per cohort), randomized 6:2 to receive YR011 or placebo in a double-blind manner. For the SAD stage, 4 dose levels are tested as a single oral dose under fasting conditions; for the MAD stage, 4 dose levels are given twice daily for 7 days plus one extra dose on Day 8. Key procedures include screening (up to 28 days before enrollment), baseline assessments, drug administration, and follow-up (7 days for SAD, 14 days for MAD). Safety is the primary endpoint (measured by treatment-related adverse events), with secondary endpoints including PK parameters (e.g., plasma concentration, half-life) and dose accumulation. Eligible participants are 18-60 years old, healthy, and able to comply with trial procedures; those with major diseases, drug allergies, or recent medication use are excluded. The trial follows ICH-GCP and FDA regulations, with a Safety Review Committee overseeing dose escalation and safety monitoring. All data is collected via electronic case report forms (eCRFs) and kept confidential.

Conditions

Safety; Tolerability; Pharmacokinetics

Keywords

KV1.3; YIRUI pharma; yirui; Healthy Volunteers

Outcome Measures

Primary Outcomes (1)

• The incidence of treatment- Emergent adverse events (TEAE)

  safety assessment will be based on the incidence of treatment- Emergent adverse events (TEAE) through out the treatment period and until the post-treatment follow-up period

  From date of randomization until the last date of the post-treatment follow-up period, up to 44 days after informed consent.

Secondary Outcomes (5)

• Plasma concentration of YR011

  During treatment period from the first dose to the last dose (up to Maximum of 10 days)

• Peak Plasma Concentration of YR011

  During treatment period from the first dose to the last dose (up to Maximum of 10 days)

• Time to peak plasma concentration of YR011

  During treatment period from the first dose to the last dose (up to Maximum of 10 days)

• Area under the plasma concentration versus time curve (AUC) of YR011

  During treatment period from the first dose to the last dose (up to Maximum of 10 days)

• Half life of YR011 (T1/2)

  During treatment period from the first dose to the last dose (up to Maximum of 10 days)

Study Arms (2)

YR011

ACTIVE COMPARATOR

Active arm: Participants receive the investigational drug YR011 at a specific dose.

Drug: Kv1.3 potassium channel blocker (PA032, investigational oral small-molecule drug)

Placebo

PLACEBO COMPARATOR

Drug: Placebo

Interventions

Kv1.3 potassium channel blocker (PA032, investigational oral small-molecule drug) DRUG

Highly selective Kv1.3 potassium channel blocker (active ingredient: PA032) - oral tablet formulation, administered as single ascending doses or multiple ascending doses (twice daily for 7 days + 1 extra dose on Day 8) under fasting conditions.

YR011

Placebo DRUG

The placebo intervention in this study is a matched oral tablet formulationcontaining inactive ingredients (e.g., excipients like microcrystalline cellulose, lactose) with no pharmacological activity.

Placebo

Eligibility Criteria

• Age: 18 Years - 60 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Participants who meet all the following criteria could be enrolled in this study:
• Written informed consent obtained from the participant in compliance with all local legal requirements.
• Male or female participant aged between 18 and 60 years (extremes included).
• Body mass index (BMI) between 18-32 kg/m2 (extremes included) and body weight less than 120 kg.
• Males must use a condom or remain abstinent during the trial and for 3 months after their last dose of study medication. And a fertile man's female partner must not try to become pregnant during the study.
• Female participants of childbearing potential must be established on a highly effective method of contraception (The recommended birth control methods are: Implantable (e.g. Implanon(r)), injectable (e.g. Depo-Provera(r)), insertable (e.g. NuvaRing®), Mirena (r) (LNG-IUS)), Combined oral contraceptives pill or progestin-only pill, Evra patch®, Intrauterine device (e.g. ParaGard(r), copper T) or Female sterilization, Male sterilization. The recommended birth control methods must be taken at least 3 weeks prior to screening (i.e., to ensure the contraceptive method has taken effect).) prior to dosing and until 3 months after their last dose in combination with male partner's use of a condom during the trial and for 3 months after the last dose.
• Free from any clinically relevant illness or disease that may adversely affect the safety of the participant, or the integrity of the study as determined by medical history, physical examination, safety laboratory, and other assessments.
• Participants must be willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other study procedures. Without other intestinal diseases such as irritable bowel syndrome and acute diarrhea due to any infection.

You may not qualify if:

• If the participants meet any of the following criteria, they cannot be enrolled in this clinical trial:
• Pregnant or lactating women.
• Participants with dysphagia.
• Severe infections requiring parenteral antibiotics treatment within 4 weeks prior to screening, e.g. sepsis, or severe pneumonia.
• Any clinically relevant conditions e.g. cerebral stroke, myocardial infarction, heart failure, unstable angina, and severe heart rate abnormalities within 6 months before screening.
• History or presence (within 6 months) of gastrointestinal, hepatic, or renal disease or any other condition known to interfere with absorption, distribution, metabolism, or excretion of drugs.
• Participant has a supine blood pressure outside the ranges of 90 to 140 mm Hg for systolic and 40 to 90 mm Hg for diastolic, confirmed with repeat per PI discretion, at the Screening Visit or Inpatient Check-in (Day -1).
• Presence of any renal impairment or dysfunction (i.e. estimated glomerular filtration rate (eGFR)\<90 mL/ min).
• Presence of hepatic impairment: Child-Pugh A, B or C and/or transaminase levels that are outside the upper normal limit (i.e., Serum bilirubin ≥1.5× upper limit of normal (ULN), ALT or AST levels \> ULN).
• diagnosis of diabetes regardless the degree of control at screening visit
• Hyperthyroidism or hypothyroidism.
• Malignancy within 5 years, except for basal or squamous cell carcinoma of the skin or carcinoma in situ of the cervix that has been successfully treated.
• Any major surgery within 6 months of screening.
• Participant has a positive test result of HBV (positive HBsAg), HCV (positive anti-HCV), or human immunodeficiency virus I and II (positive anti-HIV I/II), Treponema Pallidum antibody (positive anti-TP) at screening.
• Participants with innate or acquired immune system defects.

Sponsors & Collaborators

• Hangzhou Yirui Pharmaceutical Technology Co., Ltd: lead

Related Publications (1)

• Azam P, Sankaranarayanan A, Homerick D, Griffey S, Wulff H. Targeting effector memory T cells with the small molecule Kv1.3 blocker PAP-1 suppresses allergic contact dermatitis. J Invest Dermatol. 2007 Jun;127(6):1419-29. doi: 10.1038/sj.jid.5700717. Epub 2007 Feb 1.

  PMID: 17273162 BACKGROUND

Central Study Contacts

Kevin Wei

CONTACT

+86-751-86989512; kai.wei@yirui-pharma.com

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: TRIPLE
• Who Masked: PARTICIPANT, INVESTIGATOR, OUTCOMES ASSESSOR
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 20, 2025
• First Posted: December 16, 2025
• Study Start: April 1, 2026
• Primary Completion (Estimated): September 30, 2026
• Study Completion (Estimated): December 31, 2026
• Last Updated: December 26, 2025

Record last verified: 2025-12

Data Sharing

• IPD Sharing: Will not share