Tenofovir Alafenamide
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Also known as GS-7340GS-734003Tenofovir alafenamidaVemlidyTenofovir Alafenamide (GS-7340)
Summary
Tenofovir Alafenamide (CHEMBL2107825) is an approved small-molecule antiviral drug (ATC J05AF13) targeting TAS2R39; indicated across 12 conditions including viral infectious disease and hepatitis b virus infection.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: J05AF13
- Targets: 1 (TAS2R39)
- Indications: 12 conditions
- Clinical trials: 74
- Chemistry: 476.5 Da · C21H29N6O5P
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2107825 |
| Name | Tenofovir Alafenamide |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 9574768 |
| ChEBI | CHEBI:90926 |
| ATC | J05AF13 |
| Molecular formula | C21H29N6O5P |
| Molecular weight | 476.5 |
| InChIKey | LDEKQSIMHVQZJK-CAQYMETFSA-N |
SMILES: C[C@H](CN1C=NC2=C(N=CN=C21)N)OC[P@@](=O)(N[C@@H](C)C(=O)OC(C)C)OC3=CC=CC=C3
IUPAC name: propan-2-yl (2S)-2-[[[(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethyl-phenoxyphosphoryl]amino]propanoate
ChEBI definition: An L-alanine derivative that is isopropyl L-alaninate in which one of the amino hydrogens is replaced by an (S)-({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)(phenoxy)phosphoryl group. A prodrug for tenofovir, it is used (as the fumarate salt) in combination therapy for the treatment of HIV-1 infection.
Pharmacological roles (ChEBI): antiviral drug, HIV-1 reverse transcriptase inhibitor, prodrug.
Also known as: GS-7340, Gs-7340, GS-734003, Tenofovir alafenamida, Tenofovir alafenamide, Vemlidy, TENOFOVIR ALAFENAMIDE, Tenofovir Alafenamide, Tenofovir Alafenamide (GS-7340)
Parent form; salt/anhydrous children: CHEMBL2364637, CHEMBL5184176
Patent coverage: 983 distinct patent families (2,433 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,259 (93%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| TAS2R39 | TAS2R39 | Agonist | 0.3% | P59534 |
Bioactivity
No ChEMBL bioactivity rows at pChembl ≥ 5 (expected for biologics / antibodies).
Target pathways
Aggregated over 1 target gene(s): TAS2R39.
Top Reactome pathways
9 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | TAS2R39 |
| Signaling by GPCR | 1 | TAS2R39 |
| GPCR downstream signalling | 1 | TAS2R39 |
| G alpha (i) signalling events | 1 | TAS2R39 |
| Class C/3 (Metabotropic glutamate/pheromone receptors) | 1 | TAS2R39 |
| GPCR ligand binding | 1 | TAS2R39 |
| Sensory Perception | 1 | TAS2R39 |
| Sensory perception of taste | 1 | TAS2R39 |
| Sensory perception of sweet, bitter, and umami (glutamate) taste | 1 | TAS2R39 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| detection of chemical stimulus involved in sensory perception of bitter taste | 1 |
| signal transduction | 1 |
| G protein-coupled receptor signaling pathway | 1 |
| sensory perception of taste | 1 |
Indications & clinical
Indications
12 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| viral infectious disease | 4 | MONDO:0005108 | EFO:0000763 |
| hepatitis B virus infection | 3 | MONDO:0005344 | EFO:0004197 |
| chronic hepatitis B virus infection | 3 | MONDO:0005366 | EFO:0004239 |
| HIV infectious disease | 3 | MONDO:0005109 | EFO:0000764 |
| AIDS | 3 | MONDO:0012268 | EFO:0000765 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| B-cell chronic lymphocytic leukemia | 2 | MONDO:0004948 | EFO:0000095 |
| hepatitis D virus infection | 2 | MONDO:0005789 | EFO:0007304 |
| amyotrophic lateral sclerosis | 1 | MONDO:0004976 | MONDO:0004976 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 74.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 27 |
| Not specified | 17 |
| PHASE1 | 10 |
| PHASE2 | 9 |
| PHASE3 | 7 |
| PHASE2/PHASE3 | 2 |
| PHASE1/PHASE2 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03753074 | PHASE4 | ACTIVE_NOT_RECRUITING | Effectiveness of TAF in Reducing Clinical Events in CHB Patients Beyond Treatment Indications by Current Guidelines |
| NCT03933384 | PHASE4 | RECRUITING | Tenofovir Alafenamide Versus Entecavir for the Treatment of Chronic Hepatitis B |
| NCT04496882 | PHASE4 | ACTIVE_NOT_RECRUITING | Chronic Hepatitis b Patients Switch to tAf After Discontinuation of Nucleoside Analogue |
| NCT04619082 | PHASE4 | ACTIVE_NOT_RECRUITING | TAF to Prevent HBV Reactivation in Cancer Patients |
| NCT05410496 | PHASE4 | ACTIVE_NOT_RECRUITING | Tenofovir Alafenamide Switching Therapy in Kidney or Liver Transplant Recipients With Chronic HBV Infection |
| NCT05853718 | PHASE4 | RECRUITING | Study of Tenofovir Alafenamide in HBV-Infected Pregnant Women |
| NCT06221657 | PHASE4 | NOT_YET_RECRUITING | Clinical Trial for Non-inferiority and Safety of Tenofovir Alafenamide and Tenofovir Disoproxil Fumarate in Patients With Hematologic Malignancies Who Require Prophylactic Hepatitis B Antiviral Treatment |
| NCT06374758 | PHASE4 | RECRUITING | Accelerated ART Initiation for PWHIV Who Are Out of Care |
| NCT07476339 | PHASE4 | NOT_YET_RECRUITING | REINItiation of Antiretroviral Therapy Using Oral bicTegravir, emtrIcitAbine and Tenofovir alafenamidE |
| NCT02957864 | PHASE4 | UNKNOWN | Switching From Tenofovir Disoproxil Fumarate to Abacavir or Tenofovir Alafenamide |
| NCT03241641 | PHASE4 | COMPLETED | Switching From TDF to TAF vs. Maintaining TDF in Chronic Hepatitis B With Resistance to Adefovir or Entecavir. |
| NCT03471624 | PHASE4 | COMPLETED | Treatment Outcomes in Chronic Hepatitis B Patients on Sequential Therapy With Tenofovir Alafenamide (TAF) |
| NCT03502005 | PHASE4 | COMPLETED | Efficacy, Safety & Tolerability of Switching EFV/TDF/FTC to BIC/FTC/TAF in Virologically Suppressed Adults With HIV-1 |
| NCT03604016 | PHASE4 | UNKNOWN | Study to Assess Efficacy of Besifovir and L-carnitine in Chronic Hepatitis B Patients With Nonalcoholic Fatty Liver |
| NCT03695029 | PHASE4 | UNKNOWN | Maternal Screening and Antiviral Therapy in Pregnant Women to Reduce Mother-to-infant Transmission of Hepatitis B Virus |
| NCT03798119 | PHASE4 | UNKNOWN | TAF Switch in F3/4 CHB pt With Partial Response to NUC (ESTAB-AFPVR) |
| NCT03998176 | PHASE4 | COMPLETED | Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) in HIV-1 Infected Patients With Active Illicit Substance usE |
| NCT04070079 | PHASE4 | UNKNOWN | Tenofovir Alafenamide With Fine Needle Aspiration Biopsy in Chronic Hepatitis B: |
| NCT04132674 | PHASE4 | UNKNOWN | Switching to a Fixed Dose Combination of Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/F/TAF) in HIV-1 Infected Marginalized Populations Who Are Virologically Suppressed |
| NCT04201808 | PHASE4 | UNKNOWN | Efficacy and Safety of TAF in Patients With Suboptimal Response to Other Nucleos(t)Ides |
| NCT04636437 | PHASE4 | COMPLETED | Doravirine for Obese Persons on Integrase Inhibitors and Tenofovir Alafenamide |
| NCT04674423 | PHASE4 | UNKNOWN | The Effectiveness and Safety of Tenofovir Alafenamide in the Treatment of Chronic Hepatitis B Patients With Mildly Elevated Alanine Aminotransferase and Significant Liver Injury. |
| NCT04683341 | PHASE4 | UNKNOWN | Tenofovir Alafenamide in HBV Related Decompensated Liver |
| NCT04939441 | PHASE4 | UNKNOWN | Regression of Liver Fibrosis by Tenofovir Alafenamide (TAF) |
| NCT04997564 | PHASE4 | UNKNOWN | The Efficacy and Safety of 12-week SOF/VEL Regimen Combined With Prophylactic Use of TAF for Treatment-naïve Genotype 1-6 HCV/HBV Co-infection Adult Patients With or Without Compensated Cirrhosis in China |
| NCT05001672 | PHASE4 | UNKNOWN | The Efficacy of Prophylactic TAF for HBsAg-positive Patients Receiving bDMARDs |
| NCT05063071 | PHASE4 | UNKNOWN | Tenofovir Alafenamide for HBV Prophylaxis in Post Orthotopic Liver Transplant |
| NCT03489239 | PHASE3 | ACTIVE_NOT_RECRUITING | Entecavir to TAF Switch |
| NCT05979311 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Evaluate the Efficacy, Safety, and Tolerability of Using an Oral Once-daily 2 Drug Regimen Compared to an Oral Once-daily 3 Drug Regimen for the Treatment of Human Immunodeficiency Virus (HIV)-1 in Adults Who Have Not Previously Taken Antiretroviral Therapy |
| NCT06544733 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Study of Oral Weekly Lepetegravir (Formerly GS-1720) and Lenacapavir Pacfosacil (Formerly GS-4182) Versus Biktarvy in People With HIV-1 Who Are Virologically Suppressed |
| NCT03048422 | PHASE3 | COMPLETED | Evaluating the Efficacy and Safety of Dolutegravir-Containing Versus Efavirenz-Containing Antiretroviral Therapy Regimens in HIV-1-Infected Pregnant Women and Their Infants |
| NCT03122262 | PHASE3 | COMPLETED | ADVANCE Study of DTG + TAF + FTC vs DTG + TDF + FTC and EFV + TDF+FTC in First-line Antiretroviral Therapy |
| NCT03887702 | PHASE3 | TERMINATED | Prophylactic Antiviral Therapy in Patients With Current or Past Hepatitis B Virus Infection Receiving Anti-Cancer Therapy for Solid Tumors |
| NCT04155554 | PHASE3 | UNKNOWN | Neurological Monitoring in Patients Switching From Dolutegravir Based Regimen to Bictegravir Based Regimen |
| NCT04937881 | PHASE3 | COMPLETED | PK of TAF and TDF for PrEP in Pregnant and Postpartum Women |
| NCT06613685 | PHASE2/PHASE3 | TERMINATED | Study of Oral Weekly GS-1720 and GS-4182 Compared With Biktarvy in People With HIV-1 Who Have Not Been Treated |
| NCT05652478 | PHASE2 | RECRUITING | Early Metabolic Effects of Antiretroviral Drugs in Healthy volUnteers: a Phase 2 Randomized Study |
| NCT00036634 | PHASE1/PHASE2 | COMPLETED | A Dose Escalation Study of Tenofovir Alafenamide in Treatment-Naive Patients |
| NCT03115736 | PHASE2 | COMPLETED | TAF for HIV-HBV With Renal Dysfunction |
| NCT03804372 | PHASE2 | TERMINATED | The Incidence of Hepatitis B in Diffuse Large B-Cell Lymphoma/Chronic Lymphoid Leukemia HBsAg-positive Treated With Rituximab, Chemotherapy and Tenofovir Alafenamide |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 2 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
1 molecules share ≥1 primary target. Top 1 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | TAS2R39 |