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- ABI-H3733 / Assembly Biosci, BeiGene
Safety, pharmacokinetics, and antiviral activity of the next-generation hepatitis B core inhibitor ABI-H3733 in patients with hepatitis B e antigen negative chronic hepatitis B infection: preliminary results from a randomized, blinded, Phase 1b study (Poster Area) - Apr 12, 2023 - Abstract #EASLILC2023EASL_ILC_2071;
P1b
All AEs and lab abnormalities were Grade 1 or 2, with no serious AEs, treatment discontinuations, or deaths. No ALT elevations were observed.
- ABI-H3733 / Assembly Biosci, BeiGene, ABI-4334 / Assembly Biosci
Next generation core inhibitors ABI-H3733 and ABI-4334 have significantly improved potency and target coverage for both antiviral and cccDNA formation activities compared to first-generation core inhibitors (Poster Area) - Apr 12, 2023 - Abstract #EASLILC2023EASL_ILC_307;
3733 and 4334 are currently completing Phase 1b and Phase 1a studies, respectively. Figure: Summary of Key PK and Antiviral Properties for VBR, 3733, and 4334 Parameter VBR 300 mg QD 3733 300 mg QD 4334 300 mg QD Antiviral EC50 (nM) 281 8.8 0.5 cccDNA EC50 (nM) 3032 61 2.6 Protein adjustment (fold) 8 9.6 5.5 Plasma Cmin/paEC50 (antiviral) 1.4 127 360 Plasma Cmin/paEC50 (cccDNA) 0.1 18 69 Liver:plasma ratio 18 6 7
- || ABI-H3733 / Assembly Biosci, BeiGene
New P1 trial: A Study to Assess the Safety, Pharmacokinetics, and Antiviral Activity of ABI-H3733 in Subjects With Chronic Hepatitis B Virus Infection (clinicaltrials.gov) - Jun 10, 2022
P1b, N=50, Recruiting, Sponsor: Assembly Biosciences
- ABI-H3733 / Assembly Biosci, BeiGene
Improving the pharmacokinetic profile of the hepatitis B virus core inhibitor ABI-H3733 following oral administration: results from new formulation activities (Poster Area) - Mar 16, 2022 - Abstract #EASLILC2022EASL_ILC_1748;
Based on the relative PK data in the dog model, T2 formulation is expected to have similar 3733 exposure as the LF in humans, with predicted Cmin approximately 150- and 29-fold higher than the paEC50 for pgRNA encapsidation and cccDNA formation, respectively. The improved T2 formulation will be used in an upcoming Phase 1b study conducted with cHBV patients.
- ABI-H3733 / Assembly Biosci, BeiGene
[VIRTUAL] SAFETY AND PHARMACOKINETICS OF ABI-H3733, A NOVEL 2nd GENERATION HBV CORE PROTEIN INHIBITOR: RESULTS FROM A PHASE 1a STUDY IN HEALTHY VOLUNTEERS () - Oct 21, 2021 - Abstract #AASLD2021AASLD_1074;
Plasma concentrations exceeded in vitro EC50 values for inhibition of cccDNA formation and potent inhibition of HBV with QD dosing is projected . Additional solid dosage forms are being evaluated to provide comparable exposures to those observed with the oral liquid formulation .
- ABI-H3733 / Assembly Biosci, BeiGene, ABI-H2158 / Assembly Biosci
[VIRTUAL] Second generation Hepatitis B Virus core inhibitors ABI-H2158 and ABI-H3733 have enhanced potency and target coverage for both antiviral inhibition and covalently closed circular DNA establishment activities () - Apr 9, 2021 - Abstract #EASLILC2021EASL_ILC_1165;
VBR, 2185, and 3733 achieve plasma concentrations significantly above EC50 and paEC50 for antiviral activity. The second generation compounds 2158 and 3733 show enhanced potency and exposures that cover cccDNA prevention activity at significant multiples of paEC50 at Cmin.
- ||| ABI-H3733 / Assembly Biosci, BeiGene
Trial completion: A Study to Assess Safety, Tolerability, and Pharmacokinetics of ABI-H3733 in Healthy Adults (clinicaltrials.gov) - Jan 27, 2021
P1, N=120, Completed, Sponsor: Assembly Biosciences
The second generation compounds 2158 and 3733 show enhanced potency and exposures that cover cccDNA prevention activity at significant multiples of paEC50 at Cmin. Recruiting --> Completed
- [VIRTUAL] AMINO ACID SUBSTITUTIONS IN THE INHIBITOR BINDING POCKET OF HBV CORE PROTEIN CONFER DIFFERENTIAL CHANGES IN SUSCEPTIBILITY TO THREE GENERATIONS OF HBV CORE INHIBITORS () - Nov 2, 2020 - Abstract #AASLD2020AASLD_2141;
Although all HBV core inhibitors are known to bind the same pocket, specific amino acid substitutions in the region confer differential changes in the resistance profile of structurally distinct small molecules suggesting that specific interactions between the protein and the inhibitors modulate drug susceptibility. ETV retains activity against all tested core protein mutations suggesting that combination therapy with NrtIs may prevent viral breakthrough due to pre-existence or potential emergence of core protein substitutions.
- ||| ABI-H3733 / Assembly Biosci, BeiGene
Enrollment open, Trial completion date, Trial primary completion date: A Study to Assess Safety, Tolerability, and Pharmacokinetics of ABI-H3733 in Healthy Adults (clinicaltrials.gov) - Jun 3, 2020
P1, N=120, Recruiting, Sponsor: Assembly Biosciences
ETV retains activity against all tested core protein mutations suggesting that combination therapy with NrtIs may prevent viral breakthrough due to pre-existence or potential emergence of core protein substitutions. Not yet recruiting --> Recruiting | Trial completion date: Jul 2020 --> Nov 2020 | Trial primary completion date: Jul 2020 --> Nov 2020
- ||| ABI-H3733 / Assembly Biosci, BeiGene
New P1 trial: A Study to Assess Safety, Tolerability, and Pharmacokinetics of ABI-H3733 in Healthy Adults (clinicaltrials.gov) - Feb 16, 2020
P1, N=120, Not yet recruiting, Sponsor: Assembly Biosciences