Preliminary Human Trials of F230 Tablets

NCT06899815 | Recruiting Phase 1

• 1 other identifier: KDN-F230-202401
• Study Type: interventional
• Target: 136
• Locations: 1 country
• Sites: 1

Brief Summary

F230 is a new Class 1 chemical drug jointly developed by Beijing Contini Pharmaceutical Co., Ltd. for the treatment of pulmonary hypertension (Notification number: 2024LP01242, 2024LP01243). The in vitro activity and in vivo toxicology tests of F230, the lead compound for the treatment of PAH developed by Beijing Contini Pharmaceutical Co., LTD., showed that F230 had the same in vitro activity as the endothelin antagonist on the market. The pharmacodynamics of F230 in rats with nephrogenic hypertension induced by Sunitinib showed that F230 could reduce proteinuria and improve renal index.It is expected to bring higher treatment and survival benefits to the corresponding patients. According to the spirit of NMPA new drug approval, on the basis of the completion of preclinical studies of this drug, the safety, tolerability and pharmacokinetic characteristics of single administration and multiple administration of this drug in healthy volunteers should be investigated first, and the influence of food on the pharmacokinetic characteristics of F230 in humans should be investigated, so as to recommend a safe and effective administration regimen for phase II clinical trials.

Conditions

Pulmonary Hypertension

Keywords

Pulmonary hypertension; F230

Outcome Measures

Primary Outcomes (31)

• Single dose:PK parameters: Cmax

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: Tmax

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: AUC0-t

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: AUC0-∞

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: t1/2

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: λz

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: Vz/F

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: CL/F

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: AUC_%Extrap

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: MRT

  Blood PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: Ae_u (t1-t2)

  Urine PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: Ae_u (0-t)

  Urine PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters: Rate_u (max)

  Urine PK parameters

  Within 48 hours of dosing

• Single dose:PK parameters:Fe_u (0-t)

  Urine PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters:Cmax,ss

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters:Tmax,ss

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: AUC0-τ,ss

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: AUC0-t

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: AUC0-∞

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters:Cmin,ss

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: Cav,ss

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: t1/2

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: λz

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: CLss/F

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: AUC_%Extrap

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: MRT

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: DF

  Blood PK parameters

  Within 48 hours of dosing

• Multiple administration: PK parameters: Rac

  Blood PK parameters

  Within 48 hours of dosing

• Effects of food on single pharmacokinetic parameters: Cmax

  Blood PK parameters

  Within 48 hours of dosing

• Effects of food on single pharmacokinetic parameters: Tmax

  Blood PK parameters

  Within 48 hours of dosing

• Effects of food on single pharmacokinetic parameters: AUC

  Blood PK parameters

  Within 48 hours of dosing

Secondary Outcomes (15)

• Safety and tolerance assessment:Adverse event

  SAD: 3 days

• Safety and tolerance assessment:Adverse event

  MAD: 10 days

• Safety and tolerance assessment:Adverse event

  Effects of food on drugs test: 7 days

• Safety and tolerance assessment:Vital signs measurement：temperature

  SAD: 3 days;

• Safety and tolerance assessment:Vital signs measurement：temperature

  MAD: 10 days

Study Arms (3)

SAD single dose group

EXPERIMENTAL

A total of 6 dose groups A1-A6: F230 are initially expected to be developed (A1-A6 test groups were administered 3mg, 6mg, 12mg, 20mg, 30mg, 40mg, respectively). The specific incremental dose can be adjusted according to the test situation. The A1 dose group included 8 volunteers (stratified by sex, F230 tablets: placebo =3:1), and the A2 to A6 dose group included 14 volunteers (stratified by sex, F230 tablets: Placebo =6:1), F230 tablets or placebo were taken orally on an empty stomach on the day of administration. From the night before the start of the trial to the end of the trial evaluation period (A1:D-1 \~ D3/A2-A6:D-1 \~ D2), the volunteers were kept in the phase I research room. During the study period, safety assessment and PK biological sample collection were conducted according to the protocol. The volunteers completed a safety check on day 4(A1)or day3(A2-A6).

Drug: F230 tablets

MAD multiple dose group

EXPERIMENTAL

It is initially planned to conduct three dose groups, with preset doses of 10 mg, 20 mg, and 30 mg, Qd, administered for 7 consecutive days. Each group will include 14 volunteers (stratified by gender, F230 tablets: placebo = 6:1), with a total of 42 volunteers planned. All volunteers will stay at the research center from the day before administration (D-1) until 72 hours after the last dose (D10). During the study period, safety assessments and PK biological sample collection will be conducted according to the protocol. On the 10th day of the study (D10, 72 hours after the last dose), the procedures and related safety checks specified in the protocol will be completed. Volunteers may leave the research center only after a comprehensive evaluation by the investigator. Subsequently, volunteers will return to the research center or have a safety follow-up by phone on the 11th day of the study (D11, 96 hours after the last dose).

Drug: F230 tablets

Research on the effects of food on drugs

EXPERIMENTAL

It is planned to conduct a 20 mg dose group, with an intended enrollment of 16 volunteers. Using gender as a stratification factor, volunteers will be randomly assigned to two dosing sequence groups (K-C group and C-K group). Eight volunteers will receive the drug under fasting conditions in Period 1, while the other eight will consume a high-fat meal first and then receive the drug within 30 minutes in Period 1, with washout on Day 2. After a 3-day (72-hour) washout period, volunteers will proceed to the second dosing period on Day 6. Safety checks will be completed on study Day 7, after which volunteers may leave the research center. A safety follow-up will be conducted on Day 8.

Drug: F230 tablets

Interventions

F230 tablets DRUG

SAD： A1: F230 tablets 3mg;A2: F230 tablets 6mg;A3: F230 tablets 12mg;A4: F230 tablets 20mg;A5: F230 tablets 30mg;A6: F230 tablets 40mg . MAD： B1: F230 tablets 10mg; B2: F230 tablets 20mg; B3: F230 tablets 30mg; Studies on the effects of food on drugs:Group K-C: The first cycle was fasting administration, and the second cycle was postprandial administration;C-K:The first cycle was given after meals, and the second cycle was given on an empty stomach.

MAD multiple dose group; Research on the effects of food on drugs; SAD single dose group

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Volunteers must meet all of the following criteria to be selected:
• Healthy volunteers, half male and half female, should be replaced by volunteers of the same sex;
• Age: 18 \~ 45 years old;
• Weight: male ≥50kg, female ≥45kg, 19≤BMI≤26 (BMI= weight (kg)/height 2 (m2));
• Pass the comprehensive health examination: vital signs, physical examination, blood urine routine, blood pregnancy, blood glucose, blood lipid, blood electrolyte, hepatitis B surface antigen, liver and kidney function, hepatitis C, HIV and syphilis antibody test, 12-lead electrocardiogram, nicotine, urine drug screening, alcohol breath test, abdominal B-ultrasound, chest X-ray examination, etc., no abnormalities or abnormalities have no clinical significance;
• Before participating in the study, have a detailed understanding of the nature, significance, possible benefits, possible inconveniences and potential dangers of the trial, and voluntarily participate in this clinical trial, can communicate well with the investigators, comply with the requirements of the entire study, and have the ability to understand and sign the written informed consent.

You may not qualify if:

• Volunteers who meet one of the following conditions are not eligible for this study:
• Participants in any other clinical trial within three months prior to the trial;
• Serum ALT \> upper limit of normal (ULN), AST \> Upper limit of normal (ULN), TBil \> upper limit of normal (ULN);
• (Inquiry) Are there any underlying liver diseases, such as chronic hepatitis B, chronic hepatitis C, alcoholic liver disease, moderate to severe non-alcoholic fatty liver disease, liver cirrhosis, etc.;
• (Consultation) Have any disease that may affect the safety of the trial or the process of the drug in vivo, including but not limited to: Heart, liver, kidney, endocrine, digestive, immune, respiratory, nervous or psychiatric systems, or other pre-existing or existing diseases of the above systems \[especially cardiovascular disease including those at risk for cardiovascular disease, any gastrointestinal disease that interferes with drug absorption (e.g. symptoms of irritable bowel syndrome, history of inflammatory bowel disease), active pathological bleeding (e.g. peptic ulcer), urticaria, epilepsy, epilepsy, etc. Sensitive rhinitis, eczematous dermatitis, asthma, active pulmonary tuberculosis, etc.
• (Consultation) Allergy: If there is a history of drug, food allergy or skin allergy;
• (Interview) Any drug that inhibits or induces liver metabolism of the drug in the 28 days prior to the use of the study drug (common liver enzyme inducers: barbiturates such as phenobarbital, carbamazepine, aminomide, grofulvin, methylaminopropyl, phenytoin, Grumette, rifampin, dexamethasone; Common liver enzyme inhibitors: chlorpromazine, cimetidine, ciprofloxacin, metronidazole, chloramphenicol, isoniazid, sulfonamide);

Sponsors & Collaborators

• Beijing Continent Pharmaceutical Co, Ltd.: lead

Study Sites (1)

Union Hospital Affiliated to Tongji Medical College, Huazhong University of Science and Technology

Hubei, Wuhan, 430022, China

RECRUITING

MeSH Terms

Conditions

Hypertension, Pulmonary

Condition Hierarchy (Ancestors)

Lung Diseases; Respiratory Tract Diseases; Hypertension; Vascular Diseases; Cardiovascular Diseases

Central Study Contacts

shaojun Shi, Dr

CONTACT

027-85726085; sjshicn@163.com

Rui Zhang, Dr

CONTACT

155272727759; 392519821@qq.com

Study Design

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

Study Record Dates

• First Submitted: March 11, 2025
• First Posted: March 28, 2025
• Study Start: May 15, 2025
• Primary Completion (Estimated): July 1, 2026
• Study Completion (Estimated): July 1, 2026
• Last Updated: March 11, 2026

Record last verified: 2025-03

Data Sharing

• IPD Sharing: Will not share

Locations

CN (1)