HEC121120 / HEC Pharm - LARVOL DELTA

Improved Preclinical Drug Metabolism and Pharmacokinetics of Pibothiadine (HEC121210), a Novel Hepatitis B Virus Capsid Assembly Modulator. (PubMed, Xenobiotica) - "Pibothiadine (PBD; HEC121120) is a novel hepatitis B virus capsid assembly modulator based on GLS4 (morphothiadine) and has inhibitory activities against resistant strains.To assess the overall preclinical drug metabolism and pharmacokinetics (DMPK) properties of PBD, in vivo pharmacokinetics studies in rats and dogs have been performed along with a series of in vitro metabolism assays.The oral bioavailability of PBD in rats and dogs might be related to its medium permeability in Caco-2 cells and largely be impacted by the pH-dependent solubility. In addition, the enhanced liver/plasma exposure ratio could further increase the local exposure around the target. These improved DMPK properties might indicate better development of PBD in the clinical phase."

Journal • PK/PD data • Preclinical • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study (clinicaltrials.gov) - P1/2 | N=52 | Terminated | Sponsor: Sunshine Lake Pharma Co., Ltd. | N=126 ➔ 52 | Suspended ➔ Terminated; Company decision to discontinue trial

Enrollment change • Trial termination • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study (clinicaltrials.gov) - P1/2 | N=126 | Suspended | Sponsor: Sunshine Lake Pharma Co., Ltd. | Trial completion date: Mar 2023 ➔ Dec 2023 | Trial primary completion date: Mar 2023 ➔ Dec 2023

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

Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study (clinicaltrials.gov) - P1/2 | N=126 | Suspended | Sponsor: Sunshine Lake Pharma Co., Ltd. | Trial completion date: Sep 2022 ➔ Mar 2023 | Recruiting ➔ Suspended | Trial primary completion date: Jul 2022 ➔ Mar 2023

Trial completion date • Trial primary completion date • Trial suspension • Hepatitis B • Hepatology • Infectious Disease • Inflammation

HEC121120, a novel allosteric modulator of HBV core protein demonstrates potent antiviral activities in vitro and in vivo (EASL-ILC 2022) - "In PHH isolated from chronically infected humanized liver mouse, 14 days of GLS4 (5 μM) and HEC121120 (2 μM) treatment resulted in suppression of HBV DNA, HBsAg and HBeAg while entecavir (ETV) had no effect on either viral antigen. HEC121120 is a novel class I CAM, which demonstrated improved antiviral properties both in vitro and in vivo, further clinical study will be conducted to evaluate the antiviral potency in CHB patients."

Preclinical • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study (clinicaltrials.gov) - P1/2; N=126; Recruiting; Sponsor: Sunshine Lake Pharma Co., Ltd.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Hepatitis B • Hepatology • Infectious Disease • Inflammation

Evaluation HEC121120 Tolerance in Healthy Subjects and Patients With Chronic Hepatitis B, Pharmacokinetics Characteristics and Antiviral Activity of Ⅰ Phase of Study (clinicaltrials.gov) - P1/2; N=126; Not yet recruiting; Sponsor: Sunshine Lake Pharma Co., Ltd.

Clinical • New P1/2 trial • Hepatitis B • Hepatology • Infectious Disease