Last update 26 Jun 2024
Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
Last update 26 Jun 2024
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms B/F/TAF, BIC/FTC/TAF, Bictegravir Sodium/Emtricitabine/Tenofovir Alafenamide Fumarate + [12] |
Target |
Mechanism HIV-1 integrase inhibitors(HIV integrase inhibitors), RT inhibitors(Reverse transcriptase inhibitors) |
Therapeutic Areas |
Active Indication |
Inactive Indication- |
Originator Organization |
Active Organization |
Inactive Organization |
Drug Highest PhaseApproved |
First Approval Date US (07 Feb 2018), |
RegulationOrphan Drug (US), Overseas New Drugs Urgently Needed in Clinical Settings (CN) |
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Structure
Molecular FormulaC25H33N6O9P |
InChIKeyMEJAFWXKUKMUIR-FHPNUNMMSA-N |
CAS Registry1392275-56-7 |
View All Structures (3)
Related
88
Clinical Trials associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide FumarateAn Open-label, Single-arm Study to Provide Continued Access to Study Drug to Participants Who Have Completed Pediatric Clinical Studies Involving Gilead HIV Treatments
TruTag: Development of a Silica Microparticle Taggant System to Measure Antiretroviral Pharmacotherapy Adherence
A Double-Blind, Randomized, Placebo-Controlled Clinical Trial of Combination HIV-Specific Broadly Neutralizing Monoclonal Antibodies Combined With ART Initiation During Acute HIV Infection to Induce HIV Remission
100 Clinical Results associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
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100 Translational Medicine associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
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100 Patents (Medical) associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
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78
Literatures (Medical) associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate01 Jan 2024Heliyon
Comparison of the efficacy of combined budesonide and fexofenadine versus combined fluticasone propionate and fexofenadine on the expression of class-4 semaphorins and their receptors in the peripheral blood cells of patients with allergic rhinitis
Article
Author: Rezaei Varmaziar, Fatemeh ; Salari, Farhad ; Rezaiemanesh, Alireza ; Gorgin Karaji, Ali ; Falahi, Sara ; Feizollahi, Parisa ; Asadi, Gelayol ; Rajabinejad, Misagh ; Faryadi, Elham
Background:
Allergic rhinitis (AR) is a common immunoglobulin (Ig) E-mediated disease. This study aimed to evaluate the gene expression levels of class 4 semaphorins and their receptors in AR patients before and after treatment with budesonide and fexofenadine (B/F) compared to fluticasone propionate and fexofenadine (FP/F).
Methods:
In this study, 29 AR patients (age 34.4 ± 1.2 years, 18 men and 11 women) were treated with B/F, and 24 AR patients (age 32.8 ± 1.9 years, 15 men and 9 women) were treated with FP/F for one month. Before and after treatment, peripheral blood samples were taken from patients. The expression levels of SEMA4A, SEMA4C, SEMA4D, Plexin-B2, and Plexin-D1 genes were measured using the qPCR method. In addition, the serum levels of IgE were measured using an enzyme-linked immunosorbent assay (ELISA).
Results:
The expression levels of SEMA4A (P = 0.011), 4C (P = 0.017), Plexin-B2 (P = 0.0005), and Plexin-D1 (P = 0.008) remarkably increased in AR patients treated with B/F. Our results show a significant reduction in the gene expression levels of SEMA4A (P = 0.002), 4C (P = 0.014), 4D (P = 0.003), Plexin-B2 (P = 0.033), and Plexin-D1 (P = 0.035) after treatment with FP/F. The serum levels of IgE increased in FP/F treated group (P = 0.017) and conversely decreased in the treated group with B/F (P = 0.019). Moreover, the percentages of eosinophils were reduced in both FP/F and B/F groups (P = 0.015 and P = 0.0001, respectively).
Conclusion:
In conclusion, concomitant use of fexofenadine and fluticasone propionate reduced SEMA4A, 4C, 4D, Plexin-B2, and Plexin-D1, while the SEMA4A, 4C, Plexin-B2, and Plexin-D1 gene expression levels were increased in the patient group treated with B/F.
01 Jan 2024AIDS (London, England)
A study of the pharmacokinetics, safety, and efficacy of bictegravir/emtricitabine/tenofovir alafenamide in virologically suppressed pregnant women with HIV
Article
Author: Avihingsanon, Anchalee ; Shang, Justin ; Hindman, Jason T ; Arora, Priyanka ; Xiao, Deqing ; Davis, Maggie ; Zhang, Haeyoung ; Girish, Sandhya ; Lin, Ludwig ; Palaparthy, Ramesh ; Marathe, Dhananjay D
Objective::
The objective of this study was to assess the pharmacokinetics, safety, and efficacy and confirm the dose of once-daily bictegravir/emtricitabine/tenofovir alafenamide (BIC/FTC/TAF; B/F/TAF) during pregnancy.
Design::
An open-label, multicenter, single-arm, phase 1b study (NCT03960645) was conducted in 33 virologically suppressed pregnant women with HIV-1.
Methods::
Participants received B/F/TAF (50/200/25 mg) from the second or third trimester through ∼16 weeks postpartum. Steady-state maternal plasma pharmacokinetic samples were collected at the second and third trimesters and 6 and 12 weeks postpartum for BIC, FTC, and TAF. Neonates (n = 29) were followed from birth to 4–8 weeks with sparse washout pharmacokinetic sampling for BIC and TAF. The proportion of participants with HIV-1 RNA less than 50 copies/ml at delivery (missing = excluded) was evaluated.
Results::
Mean areas under the concentration–time curve over the dosing interval (AUCtau) for BIC, FTC, and TAF were lower during pregnancy versus postpartum but were closer to AUCtau values for nonpregnant adults with HIV reported in other studies. Geometric least-squares mean ratios for BIC, FTC, and TAF AUCtau during pregnancy versus postpartum ranged from 41 to 45%, 64 to 69% and 57 to 78%, respectively. Mean BIC trough concentrations during pregnancy were more than 6.5-fold greater than the protein-adjusted 95% effective concentration. In neonates, the median BIC half-life was 43 h. Virologic suppression was maintained in all adult participants throughout the study, with no virologic failure or treatment-emergent resistance to HIV-1, no discontinuations because of adverse events, and no perinatal transmission.
Conclusion::
Exposures to BIC, FTC, and TAF were lower during pregnancy than postpartum. However, mean BIC trough concentrations were maintained at levels indicative of efficacious exposure, and FTC/TAF data were concordant with published literature in this population. Pharmacokinetic and safety data, combined with maintenance of robust virologic suppression, suggest that once-daily B/F/TAF without dose adjustment is appropriate during pregnancy.
20 Nov 2023Chinese medical journal
Efficacy and safety profiles of dolutegravir plus lamivudine vs. bictegravir/emtricitabine/tenofovir alafenamide in therapy-naïve adults with HIV-1
Article
Author: Wang, Yanhao ; Deng, Yiming ; Wei, Yinghua ; Xu, Ruhong ; He, Lixia ; Li, Jin ; Zhong, Huijun ; Wen, Li
Abstract:
Background::
Dual regimen dolutegravir (DTG) plus lamivudine (3TC) has demonstrated non-inferior efficacy compared to DTG-based three-drug regimens (3DRs), yet directly comparative data regarding the efficacy and safety of DTG + 3TC and bictegravir/emtricitabine/tenofovir alafenamide (B/F/TAF) for therapy-naïve people with human immunodeficiency virus (HIV)-1 (PWH) are still limited. We aimed to assess the antiviral potency and safety profiles of DTG + 3TC vs. B/F/TAF based on antiretroviral therapy (ART)-naïve PWH in China.
Methods::
This retrospective multicenter study enrolled PWH initiating ART with DTG + 3TC or B/F/TAF from 2020 to 2022 in Guangdong and Guangxi. We analyzed response rates based on target not detected (TND) status using intention-to-treat (ITT) analysis. Subgroups were formed based on baseline viral load (VL) (<100,000 vs. ≥100,000 copies/mL) and CD4+ cell count (<200 vs. ≥200 cell/µL). Median time to TND VL was assessed by Kaplan–Meier method. We also measured changes from baseline in CD4+ cell counts, CD4/CD8 ratio, lipid parameters, weight, creatinine (Cr), estimated glomerular filtration rate (eGFR), and drug-related adverse effects (DRAEs).
Results::
We enrolled 280 participants, including 137 (48.9%) on DTG + 3TC and 143 (51.1%) on B/F/TAF. At week 48, 96.4% (132/137) on DTG+3TC and 100% (143/143) on B/F/TAF achieved TND (P = 0.064). At week 12, TND responses were higher with B/F/TAF (78.3% [112/143]) than DTG+3TC (30.7% [42/137]) (P <0.001). This trend held across subgroups. B/F/TAF achieved TND faster (12 weeks) than DTG+3TC (24 weeks) (P <0.001). No differences were seen in CD4+ cell count and CD4/CD8 ratio, except in the high-VL subgroup, where B/F/TAF showed better recovery. DRAEs were significantly lower with B/F/TAF (4.9% [7/143]) than with DTG + 3TC (13.1% [18/137]) (P = 0.016). Lipid parameters, body weight, and Cr increased in both groups over 48 weeks, with DTG+3TC showing a more favorable effect on triglycerides, high-density lipoprotein (HDL) cholesterol, and weight gain.
Conclusions::
In this real-life study, B/F/TAF led to a faster viral decline and fewer DRAEs compared to DTG+3TC. No significant difference was observed in the TND rate at week 48, regardless of baseline VL and CD4+ cell count. CD4+ recovery was superior for B/F/TAF in participants with high VL. The DTG + 3TC regimen had less impact on metabolic changes than B/F/TAF.
65
News (Medical) associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate30 May 2024
Drug ApprovalLicense out/inClinical Study
13 May 2024
Gene TherapyPhase 1Clinical ResultsiRNA
29 Apr 2024
Drug ApprovalPhase 1Clinical ResultPhase 2
100 Deals associated with Bictegravir/Emtricitabine/Tenofovir Alafenamide Fumarate
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
R&D Status
Approved
10 top approved records. to view more data
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| HIV Infections | US | 07 Feb 2018 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Hepatitis B | Phase 3 | - | 07 May 2018 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
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Phase 4 | HIV Infections First line | 208 | jqepmnrzia(vkmnnwgknb) = lhgdwmaavs yphzkgojuw (vgpfdoxnys ) View more | - | 02 Apr 2024 | ||
Not Applicable | - | dzzkwhscjx(xdbeiezkyy) = rqkhfbqdhb ibhfyfxjwo (lxsgsuysfd, 0.75) | - | 15 Mar 2024 | |||
dzzkwhscjx(xdbeiezkyy) = espcnbawjq ibhfyfxjwo (lxsgsuysfd, 0.62) | |||||||
Phase 3 | 243 | xusvywasxf(tbsdusrlqb) = upper respiratory tract infection (19.8% vs. 14.8%), COVID-19 (38% vs. 36.1%), pyrexia (12.4% vs. 13.1%), ALT increase (8.3% vs. 12.3%), and nasopharyngitis (12.4% vs. 6.6%). wuejhzgfeu (dhmyugvlia ) | Positive | 06 Mar 2024 | |||
Phase 2 | - | upckjguzky(qpulrxlxxn) = tvtqcegssp xlunogjpvp (enzjdrvwwr ) | Positive | 06 Mar 2024 | |||
upckjguzky(qpulrxlxxn) = fwpqjdszwh xlunogjpvp (enzjdrvwwr ) | |||||||
Phase 4 | 20 | gokcvutzud(oemjjifjjp) = ssaueuftse hogcilatmc (kovzptzgas, boqsielajw - bdhihyuvwa) View more | - | 05 Mar 2024 | |||
Phase 3 | 599 | (Group 1: DOR/ISL) | dxagvpnpmr(bjpjbsdawh) = ddzsmkwocm jyzavmciav (xfxjpvedai, jityqnsmmy - nzkvuubclj) View more | - | 21 Nov 2023 | ||
(Group 2: BIC/FTC/TAF) | dxagvpnpmr(bjpjbsdawh) = pychmlgvqu jyzavmciav (xfxjpvedai, iuaidfxadj - ehdxcofnta) View more | ||||||
Phase 4 | 28 | lrzmaapuzv(zqricinirf) = dlcfkvhfvo bntlwshpqi (bvvyhaapsr, kpxcrctioo - wvzanzjwhq) View more | - | 18 Jul 2023 | |||
Phase 4 | 20 | rdfiwrvsdq(rzitxmktxt) = soxbluudoz ddwitpeees (qbowqdomvv, dqgjwhukqp - fzemideroa) View more | - | 23 May 2023 | |||
Phase 3 | 244 | Placebo to match DTG+B/F/TAF | picxevtcbz(busqttlqmf) = twawaetmzj ttyzdvjxjz (auovubhyuj, vdcxqbwqob - wqjwsfdtmc) View more | - | 15 Mar 2023 | ||
Phase 3 | 25 | bxfghudqsm(unpxkirouj) = gtofypirrl hbseofuduo (pmziryvqtj, sculpcorsk - hisvlhyfrr) View more | - | 08 Feb 2023 |
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