Delving into the Latest Updates on Besifovir with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Besifovir dipivoxil, Besivo

+ [1]

Target

HBV pol

Mechanism

HBV pol inhibitors(HBV DNA Polymerase inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System Disorders

Active Indication

Hepatitis B, Chronic

Inactive Indication-

Originator Organization

LG Life Sciences Ltd.

Active Organization

Ildong Pharmaceutical Co., Ltd.

Inactive Organization

LG Life Sciences Ltd.

Drug Highest PhaseApproved

First Approval Date

KR (01 Mar 2017),

Hepatitis B, Chronic

Regulation-

Login to view timeline

Structure

Molecular FormulaC10H14N5O4P

InChIKeyKDNSSKPZBDNJDF-UHFFFAOYSA-N

CAS Registry441785-25-7

View All Structures (2)

Background/Aims: Four high-genetic barrier nucleos(t)ide analogues (NAs) for chronic hepatitis B (CHB), namely entecavir (ETV), tenofovir disoproxil fumarate (TDF), tenofovir alafenamide (TAF), and besifovir dipivoxil maleate (BSV), have been established. The aim of this study is to investigate the efficacy of four high-genetic barrier NAs using a network meta-analysis of randomized trials and propensity score-matched cohorts.Methods: Systematic search was performed using PubMed, Cochrane library, and EMBASE and included randomized controlled trials and cohort studies that used propensity score matching. Studies on treatment-naïve CHB patients treated with ETV, TDF, TAF, or BSV were included. Outcomes included alanine aminotransferase normalization and hepatitis B e antigen seroclearance at week 48 and undetectable hepatitis B virus DNA at weeks 48 and 96. Network meta-analysis was performed to synthesize the results.Results: In total, 15,000 patients from 16 studies were included. In terms of 48- and 96-week virologic response (VR), TDF outperformed ETV with statistical significance (48 weeks: odds ratio [OR], 1.38; p < 0.001; 96 weeks: OR, 1.57; p = 0.004). ETV was ranked first for 48-week biochemical response (BR) and outperformed TDF (OR, 0.76; p = 0.028). In the sensitivity analyses, 48-week VR from randomized-controlled trials were compiled, and the same trend toward the superiority of TDF over ETV was found (OR, 1.51; p = 0.030).Conclusions: Four high-genetic barrier NAs were compared, and TDF was more likely to achieve a VR after 48 weeks, while ETV provided a superior BR after 48 weeks.

15 Mar 2024·Gut and Liver

Noninferiority Outcomes of Besifovir Compared to Tenofovir Alafenamide in Treatment-Naïve Patients with Chronic Hepatitis B

Article

Author: Kim, Tae Hyung ; Byun, Kwan Soo ; Jung, Young Kul ; Um, Soon Ho ; Yim, Hyung Joon ; Lee, Young-Sun ; Yeon, Jong Eun ; Seo, Yeon Seok ; Kim, Ji Hoon ; Yim, Sun Young

Background/Aims: Besifovir dipivoxil maleate (BSV) and tenofovir alafenamide fumarate (TAF) have been recently approved in Korea as the initial antiviral agents for chronic hepatitis B (CHB). However, the real-world outcome data for these drugs remain limited. Therefore, we conducted a noninferiority analysis using real-world data to compare the clinical outcomes of the two nucleotide analogs in treatment-naïve patients with CHB.Methods: We retrospectively investigated a cohort of patients with CHB who received BSV or TAF as first-line antiviral agents. The endpoints were virological response (VR) and liver-related clinical outcomes.Results: A total of 537 patients, consisting of 202 and 335 patients administered BSV and TAF, respectively, were followed up for 42 months. No significant difference was observed between the VRs of the patients from the two groups. The rates of biochemical response, virologic breakthrough, and incidence rates of hepatocellular carcinoma did not differ between the groups. However, the hepatitis B e antigen seroclearance rate was higher and the renal function declined less in the BSV group. Multivariable analysis indicated older age, alcohol abuse, cirrhosis and ascites, and lower serum HBV DNA level to be independently associated with increased hepatocellular carcinoma risk. The 1:1 propensity score-matched analysis with 400 patients showed VR rates of 85.0% and 88.7% in the BSV and TAF group patients, respectively, at 2 years. The absolute value of the 95% confidence interval for the difference (-0.04 to 0.12) satisfied the a priori limit of a noninferiority of 0.15.Conclusions: BSV is noninferior to TAF in terms of VR, and their clinical outcomes are comparable to CHB.

01 Jul 2023·Alimentary pharmacology & therapeutics

Comparison of decline in renal function between patients with chronic hepatitis B with or without antiviral therapy.

Article

Author: Lee, Jae Seung ; Lee, Jung Il ; Kim, Beom Seok ; Jung, Chan-Young ; Ahn, Sang Hoon ; Kim, Seung Up

BACKGROUND AND AIMSRenal function can deteriorate in patients with chronic hepatitis B (CHB). We compared the risk of renal function decline between patients with untreated and treated CHB receiving antiviral therapy.METHODSThis retrospective study included 1061 untreated CHB patients, and 366 on tenofovir alafenamide (TAF), 190 on besifovir dipivoxil maleate (BSV), and 2029 on entecavir (ETV). The primary outcome was renal function decline, a ≥ one-stage increase in chronic kidney disease for ≥3 consecutive months.RESULTSThe incidence and risk of renal function decline were significantly higher in the 1:1 propensity score-matched treated group (588 pairs) than in the untreated (2.7 per 1000 person-years [PYs] vs. 1.3 per 1000 PYs, adjusted hazard ratio [aHR] = 2.29, all p < 0.001). The matched TAF group (222 pairs) showed a similar risk for the primary outcome (aHR = 1.89, p = 0.107) despite a significantly higher incidence thereof, compared to the untreated (3.9 vs. 1.9 per 1000 PYs, p = 0.042). The matched BSV and untreated groups (107 pairs) showed no significant differences in the incidence and risk. However, ETV users (541 pairs) carried a significantly higher outcome incidence and risk than the matched untreated (3.6 vs. 1.1 per 1000 PYs, aHR = 1.05, all p < 0.001). Compared to each matched untreated group, changes in the estimated glomerular filtration rate over time were greater in the ETV group (p = 0.010), despite being similar in the TAF (p = 0.073) and BSV groups (p = 0.926).CONCLUSIONSCompared with untreated patients, TAF or BSV users showed similar risk, whereas ETV users showed a higher risk of renal function decline.

100 Deals associated with Besifovir

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	Besifovir	J05AB	DB15671

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Hepatitis B, Chronic	KR	Ildong Pharmaceutical Co., Ltd.	01 Mar 2017

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis B, Chronic	Preclinical	CN	LG Life Sciences Ltd.	01 Aug 2009
Hepatitis B, Chronic	Preclinical	KR	LG Life Sciences Ltd.	01 Aug 2009

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01937806 (Pubmed \| Clin Mol Hepatol) Manual	Phase 3	Hepatitis B, Chronic	197	Besifovir	(ccjunrvtiz) = wgrcddmsmi bcjaywuljz (olowohdvof )	Superior	01 Apr 2021
				tenofovir disoproxil fumarate+Besifovir	(ccjunrvtiz) = eeraautcnn bcjaywuljz (olowohdvof )
NCT01937806 (Pubmed \| Clin Gastroenterol Hepatol) Manual	Phase 3	Hepatitis B, Chronic	197	Besifovir Dipivoxil Maleate	dfrujaqoip(dfntusubyw) = pziwiyxorx xlhaifwnrj (zeqhaeskdq ) View more	Similar	01 Aug 2019
				Tenofovir Disoproxil Fumarate+Besifovir	dfrujaqoip(dfntusubyw) = aabglddans xlhaifwnrj (zeqhaeskdq ) View more
NCT00895596 \| NCT01242787 (Pubmed \| Hepatology)	Not Applicable	Hepatitis B, Chronic	65	LB80380	(kgvwiyhgsw) = 44.6% of patients experienced mild and self-limiting adverse events, none of which were attributed to the study drug dqdeaafvte (ejodwwfuay )	Positive	01 Mar 2010
NCT01242787 (Pubmed \| Curr Opin Pulm Med)	Phase 1/2	Hepatitis B, Chronic	29	LB80380 30 mg	pdzmfcyxch(xkclwtinia) = uhjxtlhvae tdkcunqgpt (hwdjdrvgej )	-	01 Jan 2006
				LB80380 60 mg	pdzmfcyxch(xkclwtinia) = gmkayimnbo tdkcunqgpt (hwdjdrvgej )