Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Bictegravir · 5 trials · 3 indications
Patients will be considered non-eligible if they meet one or more of the following creiteria at week 4: * Presence of HLA-B\* 5701 or lack of HLA test * Presence of HIV genotypic resistance mutations to at least one class of ARV drug that decrease efficacy of antiretroviral treatment * CD4 count \< 200 cells/mm3 * Viral load \> 100.000 copies/mL * Comorbidities such as: Osteopenia measured by DXA (T score less than 1), medical history of cardiovascular risk measured by Framingham risk score \> 10% at 10 years, Kidney function (eGFR \<50mL/min), * Concomitant medication that can cause potential interactions with ARV (evaluating the risk of drug-drug interactions for drugs no totally safe (green colour) using the Liverpool website for DDI) * Hepatitis B (HBV) coinfection or lack of serology
AUCinf is defined as the area under the plasma concentration versus time curve extrapolated to infinite time.
Free AUCinf was calculated based on unbound plasma bictegravir (AUCinf × percentage unbound bictegravir ÷ 100 for each participant).
AUClast is defined as the area under the plasma concentration versus time curve from time zero to the last quantifiable concentration.
Free AUClast was calculated based on unbound plasma bictegravir (AUClast × percentage unbound bictegravir ÷ 100 for each participant).
Cmax is defined as the maximum observed plasma concentration of drug.
Free Cmax was calculated based on unbound plasma bictegravir (Cmax × percentage unbound bictegravir ÷ 100 for each participant).
DAVG11 was defined as the time-weighted average between the first postbaseline value through the last available on-treatment (ie, the last dose date + 1) value up to Day 11 minus the baseline value in plasma HIV-1 RNA (log10 copies/mL). All HIV-1 RNA data up to Day 11 were used for this analysis. DAVG11 was calculated using the trapezoidal rule and the area-under-the-curve concept.
| Arm | Type | Description |
|---|---|---|
| Biktarvy | EXPERIMENTAL | This is a fixed dose combination regimen containing 50 mg of Bictegravir + 200 mg of Emtricitabine + 25 mg of Tenofovir alafenamide. |
| Treatment Group 1: Bictegravir (BIC)/ Lenacapavir (LEN) (75/50 mg) + PTM B/F/TAF | EXPERIMENTAL | Blinded Phase: Participants will switch from bictegravir/emtricitabine/tenofovir (B/F/TAF) FDC tablets to BIC/LEN (75/50 mg) FDC tablets and placebo-to-match (PTM) B/F/TAF. Participants will receive a 2-day oral loading dose of LEN 600 mg on Day 1 and on Day 2, in addition to the daily doses of BIC/LEN FDC tablet starting on Day 1 up to end of blinded treatment (EBT) visit. Open-label (OL) Phase: Following treatment in the Blinded Phase, participants from Treatment Group 1 will receive BIC/LEN FDC tablets through Week 48 in the Open-label Phase. At the OL Week 48 visit, participants from Treatment Group 1 will be given the option to continue to receive BIC/LEN FDC tablets until the conclusion of the OL Phase. |
| Treatment Group 2: B/F/TAF (50/200/25 mg) + PTM BIC/LEN | EXPERIMENTAL | Blinded Phase: Participants will continue with their B/F/TAF (50/200/25 mg) FDC tablets and start PTM BIC/LEN tablets on Day 1. Participants will receive PTM LEN tablets for 2 days (2 PTM LEN tablets on Day 1 and on Day 2. The blinded phase will continue until the EBT visit. Open Label Phase: Participants in Treatment Group 2 who complete the EBT visit will be given the option to enter the OL phase to receive BIC/LEN FDC tablets until the conclusion of the OL Phase. |
| Phase 2: Bictegravir (BIC) 75 mg + Lenacapavir (LEN) 25 mg | EXPERIMENTAL | Participants will switch from their stable baseline regimen (SBR) to a regimen of BIC 75 mg + LEN 25 mg. Participants will receive a 2-day loading dose regimen of LEN 600 mg, in addition to the daily doses of BIC 75 mg + LEN 25 mg starting on Day 1 up to the end of randomized treatment (ERT) visit, participants will be treated for at least 24 weeks during the Randomized Period. Following Randomized Period, the participants will have an option to participate in an Extension Period to receive BIC/LEN 75 mg/50 mg fixed dose combination (FDC). |
| Phase 2: BIC 75 mg + LEN 50 mg | EXPERIMENTAL | Participants will switch from their SBR to a regimen of BIC 75 mg + LEN 50 mg. Participants will receive a 2-day loading dose regimen of LEN 600 mg, in addition to the daily doses of BIC 75 mg + LEN 50 mg starting on Day 1 up to the ERT visit, participants will be treated for at least 24 weeks during the Randomized Period. Following Randomized Period, the participants will have an option to participate in an Extension Period to receive BIC/LEN 75 mg/50 mg FDC. |
| Phase 2: Stable Baseline Regimen (SBR) | ACTIVE_COMPARATOR | Participants will continue with their SBR per prescription for up to the ERT visit, participants will be treated for at least 24 weeks during the Randomized Period. Following Randomized Period, the participants will have an option to participate in an Extension Period to receive BIC/LEN 75 mg/50 mg FDC. |
| Phase 3: BIC/LEN 75 mg/50 mg Fixed-dose Combination (FDC) | EXPERIMENTAL | Participants will switch from their SBR to a regimen of BIC/LEN 75 mg/50 mg FDC. Participants will receive a 2-day loading dose regimen of LEN 600 mg, in addition to the daily doses of BIC/LEN 75 mg/50 mg FDC starting on Day 1 up to the ERT visit, participants will be treated for at least 48 weeks during the Randomized Period. Following Randomized Period, the participants will have an option to participate in an Extension Period to receive BIC/LEN 75 mg/50 mg FDC. |
| Phase 3: Stable Baseline Regimen | ACTIVE_COMPARATOR | Participants will continue with their SBR per prescription for up to the ERT visit, participants will be treated for at least 48 weeks during the Randomized Period. Following Randomized Period, the participants will have an option to participate in an Extension Period to receive BIC/LEN 75 mg/50 mg FDC. |
| Severe Renal Impairment | EXPERIMENTAL | Participants with severe renal impairment and matched healthy controls will receive a single dose of bictegravir. |
| Moderate Renal Impairment | EXPERIMENTAL | Participants with moderate renal impairment and matched healthy controls will receive a single dose of bictegravir. |
| Mild Renal Impairment | EXPERIMENTAL | Participants with mild renal impairment and matched healthy controls will receive a single dose of bictegravir. |
| Bictegravir 5 mg | EXPERIMENTAL | Bictegravir 5 mg (1 × 5 mg tablet) for 10 days |
| Bictegravir 25 mg | EXPERIMENTAL | Bictegravir 25 mg (1 × 25 mg tablet) for 10 days |
| Bictegravir 50 mg | EXPERIMENTAL | Bictegravir 50 mg (2 × 25 mg tablets) for 10 days |
| Bictegravir 100 mg | EXPERIMENTAL | Bictegravir 100 mg (1 × 100 mg tablet) for 10 days |
| Placebo | PLACEBO_COMPARATOR | Placebo matched to bictegravir tablet for 10 days |
| Name | Type | Description |
|---|---|---|
| Biktarvy | DRUG | Once daily fixed dose combination regimen of Biktarvy will be evaluated as a rapid treatment strategy in newly HIV diagnosed patients HIV diagnosed patients that come for the first time to the Hospital Clínic HIV Unit |
| Bictegravir | DRUG | Tablets administered orally without regard to food |
| Lenacapavir | DRUG | Tablets administered orally without regard to food |
| B/F/TAF | DRUG | Tablets administered orally without regard to food |
| Placebo to match B/F/TAF | DRUG | Tablets administered orally without regard to food |
| Placebo to match BIC/LEN | DRUG | Tablets administered orally without regard to food |
| BIC/LEN FDC | DRUG | Tablets administered orally without regard to food |
| Stable Baseline Regimen | DRUG | SBR will include a combination of antiretroviral (ARV) regimen. ARV regimen may include the following, except for participants taking a single tablet regimen or taking a complete parenteral regimen (Cabenuva). * Nucleos(t)ide Reverse Transcriptase Inhibitors: * Abacavir * Emtricitabine * Lamivudine * Tenofovir alafenamide * Tenofovir disoproxil fumarate * Zidovudine * Non-Nucleosite Reverse Transcriptase Inhibitors: * Delavirdine * Efavirenz * Nevirapine * Rilpivirine * Doravirine * Integrase Inhibitors: * Bictegravir * Cabotegravir * Dolutegravir * Elvitegravir * Raltegravir * Protease Inhibitors: * Atazanavir * Darunavir * Fosamprenavir * Indinavir * Lopinavir * Nelfinavir * Saquinavir * Tipranavir * Chemokine Co-receptor 5 (CCR5) Antagonist: * Maraviroc * Fusion Inhibitors: * Enfuvirtide * gp120 Attachment Inhibitor: * Fostemsavir * Anti-CD4 Monoclonal Antibodies: * Ibalizumab-uiyk |
| Placebo | DRUG | Placebo to match bictegravir administered orally once daily |
Inclusion Criteria: 1. Age ≥ 18 years old. 2. Having confirmed HIV-1 positive test. 3. Patients not previously treated with antiretroviral treatment (post-exposure prophylaxis will be allowed if not done in the previous 6 months). 4. Clinically stable patients, in the opinion of the investigator, a...
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Bictegravir is an investigational small molecule being developed for the treatment of HIV, specifically HIV-1 infection. It is studied in combination with other antiretroviral agents, including emtricitabine and tenofovir alafenamide, as well as lenacapavir, for managing HIV-1 in infected adults.
Bictegravir is an integrase strand transfer inhibitor that targets the HIV-1 integrase enzyme, blocking viral DNA integration into host cells. This mechanism disrupts the HIV replication cycle, reducing viral load in infected individuals.
Bictegravir is developed by Gilead Sciences, Inc., a biopharmaceutical company traded on NASDAQ under the ticker GILD. Gilead is conducting clinical trials to evaluate the drug's safety and efficacy in treating HIV-1 infection.
Bictegravir is in Phase 1 clinical development, with early studies assessing safety, pharmacokinetics, and antiviral activity. It remains investigational and has not been approved by regulatory authorities for commercial use.
Bictegravir is being studied in several trials, including NCT02275065, a completed Phase 1 study evaluating safety and antiviral activity in HIV-1 infected participants, and NCT02400307, a completed pharmacokinetic study in adults with normal and impaired renal function. Additional trials are ongoing.
Bictegravir is a component of the combination product bictegravir/emtricitabine/tenofovir alafenamide, which is also known as Biktarvy. While bictegravir alone is the active integrase inhibitor, the combination includes two additional antiretroviral drugs for enhanced efficacy.