ASC42 / Ascletis - LARVOL DELTA

Study to Evaluate the Safety and Efficacy of ASC42 Tablets in Subjects With Primary Biliary Cholangitis (clinicaltrials.gov) - P2 | N=98 | Completed | Sponsor: Gannex Pharma Co., Ltd. | Recruiting ➔ Completed | Trial completion date: Nov 2023 ➔ Mar 2024 | Trial primary completion date: Nov 2023 ➔ Mar 2024

Trial completion • Trial completion date • Trial primary completion date • Hepatology • Immunology • Primary Biliary Cholangitis

Study to Evaluate Safety and Efficacy of ASC42 Combined With ETV and PEG-IFN α-2a in Subjects With HBV (clinicaltrials.gov) - P2 | N=43 | Completed | Sponsor: Ascletis Pharmaceuticals Co., Ltd. | Active, not recruiting ➔ Completed | Trial completion date: Feb 2023 ➔ Dec 2023 | Trial primary completion date: Feb 2023 ➔ Nov 2023

Combination therapy • Trial completion • Trial completion date • Trial primary completion date • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Drug Interaction Study of ASC42 With Atorvastatin (clinicaltrials.gov) - P1 | N=12 | Completed | Sponsor: Gannex Pharma Co., Ltd. | Recruiting ➔ Completed

Trial completion

Human Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASC42, a Novel Farnesoid X Receptor Agonist. (PubMed, Drugs R D) - P1 | "ASC42 was well tolerated with a pharmacokinetic profile suitable for QD dosing, and demonstrated dose-dependent targets engagement without altering plasma cholesterol in healthy subjects."

Journal • PK/PD data • Addiction (Opioid and Alcohol) • Atrial Fibrillation • Cardiovascular • Dermatology • Fibrosis • Hepatology • Immunology • Non-alcoholic Fatty Liver Disease • Non-alcoholic Steatohepatitis • Primary Biliary Cholangitis • Pruritus • FGF19

A phase 2 study of ASC42, a novel farnesoid X receptor (FXR) agonist, in combination with PEGylated interferon (PEG-IFN) and entecavir（ETV) in chronic hepatitis B patients with 12-week treatment (EASL-ILC 2023) - P2 | "Background and Aims: ASC42 is a novel non-steroidal, selective, potent farnesoid X receptor (FXR) agonist. As a novel FXR agonist, 10 mg ASC42 in combination of PEG-IFN-α-2a and ETV, was safe and well-tolerated and showed minimum and mild pruritus (13.3%) in Chinese CHB patients with a 4-fold safety margin and better efficacy biomarker 7α-hydroxy-4-cholesten-3-one (C4) inhibition (67%) than obeticholic acid (OCA) at 10-50 mg (40.1-47.3%)."

Clinical • Combination therapy • P2 data • Dermatitis • Dermatology • Hepatitis B • Hepatology • Infectious Disease • Inflammation • Liver Failure • Pruritus • IFNA1

Study to Evaluate the Safety and Efficacy of ASC42 Tablets in Subjects With Primary Biliary Cholangitis (clinicaltrials.gov) - P2 | N=100 | Recruiting | Sponsor: Gannex Pharma Co., Ltd. | Trial completion date: Sep 2022 ➔ Nov 2023 | Trial primary completion date: Aug 2022 ➔ Nov 2023

Trial completion date • Trial primary completion date • Hepatology • Immunology • Primary Biliary Cholangitis

Study to Evaluate Safety and Efficacy of ASC42 Combined With ETV and PEG-IFN α-2a in Subjects With HBV (clinicaltrials.gov) - P2 | N=43 | Active, not recruiting | Sponsor: Ascletis Pharmaceuticals Co., Ltd. | Recruiting ➔ Active, not recruiting

Combination therapy • Enrollment closed • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Drug Interaction Study of ASC42 With Atorvastatin (clinicaltrials.gov) - P1 | N=12 | Recruiting | Sponsor: Gannex Pharma Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open

Drug Interaction Study of ASC42 With Atorvastatin (clinicaltrials.gov) - P1 | N=12 | Not yet recruiting | Sponsor: Gannex Pharma Co., Ltd.

New P1 trial

Study to Evaluate Safety, Tolerability and Pharmacokinetics of ASC42 in Chinese Healthy Subjects (clinicaltrials.gov) - P1 | N=30 | Completed | Sponsor: Ascletis Pharmaceuticals Co., Ltd. | Active, not recruiting ➔ Completed | Trial completion date: Feb 2022 ➔ Aug 2021

Trial completion • Trial completion date

Study to Evaluate the Safety and Efficacy of ASC42 Tablets in Subjects With Primary Biliary Cholangitis (clinicaltrials.gov) - P2 | N=100 | Recruiting | Sponsor: Gannex Pharma Co., Ltd. | Not yet recruiting ➔ Recruiting

Enrollment open • Hepatology • Immunology • Primary Biliary Cholangitis

Study to Evaluate Safety and Efficacy of ASC42 Combined With ETV and PEG-IFN α-2a in Subjects With HBV (clinicaltrials.gov) - P2 | N=45 | Recruiting | Sponsor: Ascletis Pharmaceuticals Co., Ltd. | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Study to Evaluate the Safety and Efficacy of ASC42 Tablets in Subjects With Primary Biliary Cholangitis (clinicaltrials.gov) - P2; N=100; Not yet recruiting; Sponsor: Gannex Pharma Co., Ltd.

Clinical • New P2 trial • Hepatology • Immunology • Primary Biliary Cholangitis

Ascletis Announces First Patient Dosed in the Phase II Clinical Trial of ASC42, An In-House Developed, Best-in-Class FXR Agonist for Chronic Hepatitis B Indication (PRNewswire) - "Ascletis Pharma Inc...today announces the dosing of the first patient in the Phase II clinical trial of ASC42 for chronic hepatitis B (CHB) indication. The Phase II clinical trial...is a multi-center, randomized, single-blind, placebo-controlled study in China to evaluate safety and efficacy of ASC42 tablets in combination with Entecavir and pegylated interferon-α-2a (PEG-IFN-α-2a) in subjects with CHB. About 45 CHB patients will be enrolled...serum hepatitis B surface antigen (HBsAg) and hepatitis B virus (HBV) pregenomic RNA (pgRNA) change from baseline will be measured during 12-week intervention period and 24-week follow-up period."

Trial status • Hepatitis B • Infectious Disease

Safety, Tolerability, and Pharmacokinetics of ASC43F, a Fixed Dose Combination Tablet in Healthy Subjects (clinicaltrials.gov) - P1; N=8; Recruiting; Sponsor: Gannex Pharma Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open

Safety, Tolerability, and Pharmacokinetics of ASC43F, a Fixed Dose Combination Tablet in Healthy Subjects (clinicaltrials.gov) - P1; N=8; Not yet recruiting; Sponsor: Gannex Pharma Co., Ltd.

Clinical • New P1 trial

Study to Evaluate Safety and Efficacy of ASC42 Combined With ETV and PEG-IFN α-2a in Subjects With HBV (clinicaltrials.gov) - P2; N=45; Not yet recruiting; Sponsor: Ascletis Pharmaceuticals Co., Ltd.

Clinical • Combination therapy • New P2 trial • Hepatitis B • Hepatology • Infectious Disease • Inflammation

[VIRTUAL] ASC42, A NOVEL NON-STEROIDAL FXR AGONIST, DEMONSTRATES A NORMAL CHOLESTEROL PROFILE AND LACK OF PRURITUS AT THERAPEUTIC DOSES IN A 14- DAY PHASE I RANDOMIZED, DOUBLE-BLIND, PLACEBO CONTROLLED STUDY IN HEALTHY VOLUNTEERS (AASLD 2021) - P1 | "ASC42 for 14-days was well tolerated and safe, without pruritus, elevated ALT/AST or lipid parameter abnormalities at doses within the therapeutic dose range . ASC42 potently suppressed C4 plasma levels and transiently induced FGF-19 plasma levels . These data support advancement of ASC42 into the indication of NASH ."

Clinical • P1 data • Dermatology • Hepatology • Non-alcoholic Steatohepatitis • Pruritus • FGF19

[VIRTUAL] ASC43F TABLET AS A ONE-PILL, ONCE-A-DAY FIXED-DOSE COMBINATION (FDC) OF ASC41, A THR-Β AGONIST, AND ASC42, AN FXR AGONIST, DEMONSTRATED COMPARABLE DISSOLUTION PROFILES AND IN VIVO PHARMACOKINETICS VS. SINGLE ASC41 AND ASC42 TABLET (AASLD 2021) - "ASC43F is a One-Pill, Once-a-Day FDC of THR-β agonist and FXR agonist for NASH treatment and will improve patient compliance ."

PK/PD data • Preclinical • Dermatology • Hepatology • Non-alcoholic Steatohepatitis • Pruritus • FGF19

Study to Evaluate Safety, Tolerability and Pharmacokinetics of ASC42 in Chinese Healthy Subjects (clinicaltrials.gov) - P1; N=30; Active, not recruiting; Sponsor: Ascletis Pharmaceuticals Co., Ltd.; Trial completion date: Sep 2021 ➔ Feb 2022

Clinical • Trial completion date

Ascletis Announces Completion of the Bridging Study and Initiation of Phase II Trial of FXR Agonist ASC42 in China for Chronic Hepatitis B Indication (PRNewswire) - P1, N=30; NCT04965337; Sponsor: Ascletis Pharmaceuticals Co., Ltd.; "Ascletis Pharma Inc...announces today the completion of the bridging study and initiation of Phase II trial of farnesoid X receptor (FXR) agonist ASC42 in China for chronic hepatitis B (CHB) indication...ASC42 bridging study demonstrated consistent pharmacokinetic profiles between the U.S. and Chinese population...10 mg and 15 mg once daily doses of ASC42 were selected in combination with pegylated interferon and nucleos(t)ides analogs for Phase II study in Chinese patients with CHB."

P1 data • PK/PD data • Trial completion • Trial status • Hepatitis B • Infectious Disease

Study to Evaluate Safety, Tolerability and Pharmacokinetics of ASC42 in Chinese Healthy Subjects (clinicaltrials.gov) - P1; N=30; Active, not recruiting; Sponsor: Ascletis Pharmaceuticals Co., Ltd.; Recruiting ➔ Active, not recruiting

Clinical • Enrollment closed

Study to Evaluate Safety, Tolerability and Pharmacokinetics of ASC42 in Chinese Healthy Subjects (clinicaltrials.gov) - P1; N=30; Recruiting; Sponsor: Ascletis Pharmaceuticals Co., Ltd.; Not yet recruiting ➔ Recruiting

Enrollment open

Study to Evaluate Safety, Tolerability and Pharmacokinetics of ASC42 in Chinese Healthy Subjects (clinicaltrials.gov) - P1; N=30; Not yet recruiting; Sponsor: Ascletis Pharmaceuticals Co., Ltd.

Clinical • New P1 trial

Ascletis Announces Dosing of the First Cohort of Healthy Subjects in the FXR Agonist ASC42 Bridging Study for Chronic Hepatitis B Indication in China (PRNewswire) - "Ascletis Pharma...announces the dosing of the first cohort of healthy subjects in the ASC42 bridging study in China for CHB indication...Based on the pharmacokinetic data from the ASC42 Phase I trial in 64 healthy subjects in the U.S., the bridging study in China is a randomized, placebo-controlled, double-blind single-ascending dose (5 mg and 15 mg) study in 30 healthy subjects receiving ASC42 or matching placebo..."

Trial status • Hepatitis B • Infectious Disease