Table 1.
Summary of medications that may be implemented in regimens for heavily treatment-experienced patients with HIV.
| Medication | Class | Mechanism of action | Key resistance mutations | Administration route | Trials of note |
|---|---|---|---|---|---|
| Tenofovir alafenamide (TAF) | Nucleotide reverse transcriptase inhibitor | Inhibits reverse transcription by incorporating into HIV DNA and causing chain termination | K65R | Oral | |
| Etravirine (ETR) | Non-nucleoside reverse transcriptase inhibitor | Inhibits reverse transcription by binding reverse transcriptase | L100I, K101P, V106A, E138A, V179F, Y181I/C/V, G190C, M230L | Oral | DUET 1 and 2 |
| Doravirine (DOR) | Non-nucleoside reverse transcriptase inhibitor | Inhibits reverse transcription by binding reverse transcriptase | V106A, E138K, P225H F227C | Oral | DRIVE FORWARD; DRIVE AHEAD; ILLUMINATE |
| Darunavir/ritonavir (DRV/r) | Protease inhibitor | Prevents cleavage of proteins after transcription by binding protease | V11I, V32I, L33F, I47V, I50V, I54L/M, G73S, L76V, I84V, L89V | Oral | POWER 1, 2, 3 |
| Dolutegravir (DTG) | Integrase strand inhibitor | Prevents viral DNA from incorporating with host DNA by blocking integrase | G118R, Q148H/K/R, R263K | Oral | SAILING; VIKING-3 |
| Fostemsavir (FTR) | Attachment inhibitor | Prevents HIV attachment to CD4 cells by binding to glycoprotein 120 on viral envelope | No commercially available resistance test | Oral | BRIGHTE |
| Ibalizumab (IBA) | Post-attachment inhibitor | Monoclonal antibody; binds CD4 receptor after HIV attachment and prevents fusion | No commercially available resistance test | Intravenous | TMB-301 |
| Enfuvurtide (T-20) | Fusion inhibitor | Prevents viral fusion by binding glycoprotein 41 on viral envelope | G36D/E/S, I37T/N/V, V38A/E/M, Q39R, Q40H, N42T, N43D/K/S | Subcutaneous | TORO 1 and 2 |
| Maraviroc (MVC) | CCR5 coreceptor antagonist | Binds CCR5 coreceptor on CD4 cells and prevents viral entry | CXCR4 or dual tropic virus | Oral | MOTIVATE 1 and 2 |
| Islatravir (ISL)a | Nucleoside reverse transcriptase translocation inhibitor | Inhibits translocation of viral RNA into DNA via multiple mechanisms | Data under development | Oral | Protocol 011; ILLUMINATE |
| Lenacapavir (LEN)a | Capsid inhibitor | Inhibits viral assembly, disassembly and transport through p24 protein binding | No commercially available resistance test | Subcutaneous/oral | CALIBRATE; CAPELLA |
a
These medications have not yet been approved by the FDA. Information is subject to change.