Study to Evaluate Safety, Tolerability and Pharmacokinetics of CS060380 in Healthy and Elevated LDL-C Subjects

NCT06573528 | Completed Phase 1 FDA Drug

• 1 other identifier: CS060380-FIH-CN-I-01
• Study Type: interventional
• Target: 104
• Locations: 1 country
• Sites: 1

Brief Summary

Study to Evaluate Safety, Tolerability and Pharmacokinetics of CS060380 in Healthy and Elevated LDL-C Subjects.

Conditions

MASH

Outcome Measures

Primary Outcomes (1)

• AE

  occurrence rate of AEs

  Day1 to Day 28

Secondary Outcomes (18)

• Single-Dose Pharmacokinetic (PK) Parameter (AUC0-∞)

  Day 1, day 2, day3, day4.

• Single-Dose Pharmacokinetic (PK) Parameter (AUC0-last)

  Day 1, day 2, day3, day4.

• Single-Dose Pharmacokinetic (PK) Parameter (Cmax)

  Day 1, day 2, day3, day4.

• Single-Dose Pharmacokinetic (PK) Parameter (Tmax)

  Day 1, day 2, day3, day4.

• Single-Dose Pharmacokinetic (PK) Parameter (T1/2)

  Day 1, day 2, day3, day4.

Other Outcomes (12)

• Pharmacodynamic (PD) Characteristics (Fasting serum LDL-C)

  Day 1, day 3, day 5, day 7, day 14, day 15, day 17.

• Pharmacodynamic(PD) Characteristics (HDL-C)

  Day 1, day 3, day 5, day 7, day 14, day 15, day 17.

• Pharmacodynamic (PD) Characteristics (TG)

  Day 1, day 3, day 5, day 7, day 14, day 15, day 17.

Study Arms (13)

Cohort A1: 0.2 mg CS060380

EXPERIMENTAL

Eight healthy subjects were randomly assigned to take 0.2 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo (About 240L of water on an empty stomach).

Drug: CS060380

Cohort A2: 1 mg CS060380

EXPERIMENTAL

Eight healthy subjects were randomly assigned to take 1 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo (About 240L of water on an empty stomach).

Drug: CS060380

Cohort A3: 2 mg CS060380

EXPERIMENTAL

Eight healthy subjects were randomly assigned to take 2 mg of CS060380 or placebo on day 1, Six of the subjects were on study drug and two on placebo (About 240L of water on an empty stomach). Followed by a 10 day washout period, subjects in fed state will receive the same single oral dose of CS060380 2mg or placebo on day 11.

Drug: CS060380

Cohort A4: 5 mg CS060380

EXPERIMENTAL

Eight healthy subjects were randomly assigned to take 5 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo (About 240L of water on an empty stomach).

Drug: CS060380

Cohort A5: 10 mg CS060380

EXPERIMENTAL

Eight healthy subjects were randomly assigned to take 10 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo (About 240L of water on an empty stomach).

Drug: CS060380

Cohort B1: 1 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 1 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort B2: 2 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 2 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort C1: 0.25 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.25 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort C2: 0.5 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.5 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort C3: 0.75 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.75 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort D1: 0.1 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.1 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort D2: 0.15 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.15 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Cohort D3: 0.2 mg CS060380

EXPERIMENTAL

Elevated LDL-C subjects were randomly assigned to take 0.2 mg of CS060380 or placebo, Six of the subjects were on study drug and two on placebo once daily for a consecutive 14 days.

Drug: CS060380

Interventions

CS060380 DRUG

Tablets administered orally

Also known as: Placebo

Cohort A1: 0.2 mg CS060380; Cohort A2: 1 mg CS060380; Cohort A3: 2 mg CS060380; Cohort A4: 5 mg CS060380; Cohort A5: 10 mg CS060380; Cohort B1: 1 mg CS060380; Cohort B2: 2 mg CS060380; Cohort C1: 0.25 mg CS060380; Cohort C2: 0.5 mg CS060380; Cohort C3: 0.75 mg CS060380; Cohort D1: 0.1 mg CS060380; Cohort D2: 0.15 mg CS060380; Cohort D3: 0.2 mg CS060380

Eligibility Criteria

• Age: 18 Years - 65 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• SAD
• Sign and date the ICF.
• Signing ICF age≥18 years≤55 years, male or female.
• Weight: Male≥50kg, female≥45kg BMI: 18\~28kg/m².
• Female or male subjects must be eligible for contraception during the study.
• Normal renal function.
• Good general health.
• No significant medical history, in good general health as assessed by the study during the Screening Period and no more than 28 days from the first dose.
• Understand and comply with study procedures and limitations.
• MAD
• Sign and date the ICF.
• Signing ICF age≥18 years≤65 years, male or female.
• Weight: Male≥50kg, female≥45kg BMI: 18\~35kg/m², including at least 25% of overweight subjects ( BMI : 25\~30 kg/m² ), and at least 25% of obese subjects (BMI≥ 30 kg/m² ).
• Screening period, fasting LDL-C \> 110 mg/dL (2.85 mmol/L).
• Female or male subjects must be eligible for contraception during the study.

You may not qualify if:

• SAD
• Special dietary requirements, not following a uniform diet.
• Pregnant or nursing females or females who have pregnancy plans during the trial or within 3 months after the trial.
• History of febrile illness or active infection within 7 days prior to first dose.
• Positive urine drug screening results.
• History of drug/substance abuse experiments within the past 5 years prior to the start, The baseline drug screening result is positive.
• History of previous corrected QT interval (QTc) prolongation:
• Screening periods QTcF ≥ 450 ms.
• Family history of hypocalcaemia or long QT interval syndrome.
• Use of drugs causing QT/QTc prolongation.
• Investigator judgement of clinically significant abnormal ECG results.
• Abnormal liver function: AST, ALT, ALP, GGT and TBIL\>ULN.
• Smoking or use of nicotine products within 3 months prior to screening and during the study period.
• Use of other investigational drugs 40 days prior to enrolment or within at least 5 half-lives of drug use.
• Positive screening results for infectious diseases during the screening period, include HIV, HBsAg, HBcAb, HCV antibody tests.

Sponsors & Collaborators

• Cascade Pharmaceuticals, Inc: lead

Study Sites (1)

Shanghai Xuhui Central Hospital

Shanghai, China

Location

Study Officials

• Yun Liu

  Shanghai Xuhui Central Hospital

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: DOUBLE
• Who Masked: PARTICIPANT, INVESTIGATOR
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: OTHER
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 19, 2024
• First Posted: August 27, 2024
• Study Start: September 3, 2024
• Primary Completion: May 9, 2025
• Study Completion: May 21, 2025
• Last Updated: August 13, 2025

Record last verified: 2025-08

Locations

CN (1)