Lamivudine
drugOn this page
Also known as 3TCBCH 189, (-)-EpivirEpivir-hbvGR 109714XGR-109714XGR109714XLamivudinaLamivudine component of /zidovudine tevaLamivudine component of cimduoLamivudine component of combivirLamivudine component of delstrigoLamivudine component of dovatoLamivudine component of dutrebisLamivudine component of epzicomLamivudine component of kivexaLamivudine component of symfiLamivudine component of temixysLamivudine component of triumeq
Summary
Lamivudine (CHEMBL141) is an approved small-molecule HIV-1 reverse transcriptase inhibitor (ATC J05AF05); indicated across 23 conditions including chronic hepatitis b virus infection and hiv infectious disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: J05AF05
- Indications: 23 conditions
- Clinical trials: 429
- Chemistry: 229.26 Da · C8H11N3O3S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL141 |
| Name | Lamivudine |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 3877 |
| ChEBI | CHEBI:63577 |
| ATC | J05AF05 |
| Molecular formula | C8H11N3O3S |
| Molecular weight | 229.26 |
| InChIKey | JTEGQNOMFQHVDC-UHFFFAOYSA-N |
SMILES: C1C(OC(S1)CO)N2C=CC(=NC2=O)N
IUPAC name: 4-amino-1-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one
ChEBI definition: A monothioacetal that consists of cytosine having a (2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl moiety attached at position 1. An inhibitor of HIV-1 reverse transcriptase, it is used as an antiviral in the treatment of AIDS and hepatitis B.
Pharmacological roles (ChEBI): HIV-1 reverse transcriptase inhibitor, antiviral drug, anti-HBV agent, allergen, prodrug, EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor.
Also known as: 3TC, BCH 189, (-)-, Epivir, Epivir-hbv, GR 109714X, GR-109714X, GR109714X, Lamivudina, Lamivudine, Lamivudine component of /zidovudine teva, Lamivudine component of cimduo, Lamivudine component of combivir
Parent form; salt/anhydrous children: CHEMBL537885
Patent coverage: 3,794 distinct patent families (12,250 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Microtubule-associated protein tau, Prelamin-A/C, Voltage-gated L-type calcium channel, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Albumin, Heat shock factor protein 1.
Bioactivity
ChEMBL activities: 2 potent at pChembl ≥ 5 of 6 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P38532 | 6.54 | EC50 | 287 | nM | CHEMBL_ACT_4306447 |
| MAPT | 5.45 | Potency | 3548 | nM | CHEMBL_ACT_4514627 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
23 indications (9 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 |
|---|---|---|---|
| chronic hepatitis B virus infection | 4 | MONDO:0005366 | EFO:0004239 |
| HIV infectious disease | 4 | MONDO:0005109 | EFO:0000764 |
| hepatitis B virus infection | 4 | MONDO:0005344 | EFO:0004197 |
| viral infectious disease | 4 | MONDO:0005108 | EFO:0000763 |
| hepatitis | 4 | MONDO:0002251 | HP:0012115 |
| autoimmune disease | 4 | MONDO:0007179 | MONDO:0021094 |
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| AIDS | 3 | MONDO:0012268 | EFO:0000765 |
| cirrhosis of liver | 3 | MONDO:0005155 | EFO:0001422 |
| diarrheal disease | 3 | MONDO:0001673 | HP:0002014 |
| HIV-associated nephropathy | 3 | MONDO:0005798 | EFO:0007313 |
| tuberculosis | 3 | MONDO:0018076 | MONDO:0018076 |
| Kaposi’s sarcoma | 2 | MONDO:0005055 | EFO:0000558 |
| lymphoma | 2 | MONDO:0005062 | EFO:0000574 |
| non-Hodgkin lymphoma | 2 | MONDO:0018908 | EFO:0005952 |
| tropical spastic paraparesis | 2 | MONDO:0008039 | EFO:0007527 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| Alzheimer disease | 1 | MONDO:0004975 | MONDO:0004975 |
| glioma | 1 | MONDO:0021042 | MONDO:0100342 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 429.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 122 |
| PHASE4 | 107 |
| PHASE2 | 84 |
| Not specified | 66 |
| PHASE1 | 30 |
| PHASE1/PHASE2 | 12 |
| PHASE2/PHASE3 | 6 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05393193 | PHASE4 | ACTIVE_NOT_RECRUITING | POC HIV Testing and Early DTG Use for Infants |
| NCT05493969 | PHASE4 | NOT_YET_RECRUITING | Efficacy and Tolerability of DTG Plus 3TC in HIV Infected Adults With Virologically Suppression and TDF Toxicity |
| NCT06037564 | PHASE4 | ENROLLING_BY_INVITATION | B-free Multistage Trial |
| NCT06485154 | PHASE4 | ACTIVE_NOT_RECRUITING | Post-Injectable Cabotegravir Antiretroviral Salvage Strategy Options Trial |
| NCT06503796 | PHASE4 | NOT_YET_RECRUITING | Antiviral Therapy in Infants With HBV Infection |
| NCT06602622 | PHASE4 | RECRUITING | Change in Body Weight and BMI in PWH with DOR/3TC/TDF Compared with INSTI |
| NCT06967753 | PHASE4 | RECRUITING | Switch to Dolutegravir Plus Lamivudine Dual-Therapy in Transgender Women Living With HIV on Virologically Suppressive Antiretroviral Therapy (TRANS-SWITCH) |
| NCT07031063 | PHASE4 | RECRUITING | Safety, Tolerability and Effectiveness of DTG/3TC vs BIC/TAF/FTC in PWH Without Antiretroviral Experience |
| NCT07357584 | PHASE4 | NOT_YET_RECRUITING | Efficacy and Safety of Doravirine in the Rapid Initiation |
| NCT00002179 | PHASE4 | COMPLETED | The Effectiveness of Indinavir Plus Zidovudine Plus Lamivudine in HIV-Infected Patients With No Symptoms of Infection |
| NCT00002376 | PHASE4 | COMPLETED | The Effectiveness of HIV RNA Viral Load Testing in Determining Treatment Type in HIV-Infected Patients |
| NCT00002386 | PHASE4 | COMPLETED | Effect of Indinavir Plus Two Other Anti-HIV Drugs on Blood Clotting in HIV-Positive Males With Hemophilia |
| NCT00004585 | PHASE4 | COMPLETED | A Study of the Safety and Effectiveness of Combination Anti-HIV Therapy in HIV-Infected Adults |
| NCT00005000 | PHASE4 | UNKNOWN | Treatment With Nelfinavir or Efavirenz of HIV-Infected Patients Who Have Never Received Anti-HIV Drugs |
| NCT00005017 | PHASE4 | UNKNOWN | Effectiveness and Safety of Epivir/Ziagen/Zerit (3TC/ABC/d4T) Versus Epivir/Ziagen/Sustiva (3TC/ABC/EFV) Versus Epivir/Ziagen/Agenerase/Norvir (3TC/ABC/APV/RTV) in HIV Patients Who Have Never Received Treatment |
| NCT00005106 | PHASE4 | COMPLETED | A Comparison of Three Anti-HIV Drug Combinations in HIV-Infected Patients |
| NCT00005764 | PHASE4 | COMPLETED | A Study of Increased Lactic Acid and Abnormal Fat Distribution in HIV-Positive Patients |
| NCT00006190 | PHASE4 | COMPLETED | A Study to Determine How and Why HIV-Infected Subjects on Anti-viral Treatment Develop Lipodystrophy |
| NCT00038506 | PHASE4 | COMPLETED | Study Of Investigational Regimen Combining FDA Approved HIV Drugs In HIV Subjects Experiencing Early Virologic Failure |
| NCT00084136 | PHASE4 | COMPLETED | Prospective Evaluation of Anti-retroviral Combinations for Treatment Naive, HIV Infected Persons in Resource-limited Settings |
| NCT00084253 | PHASE4 | COMPLETED | Study of Boosted Atazanavir (ATV) Versus Non-boosted ATV in Naive Patients |
| NCT00116116 | PHASE4 | COMPLETED | DART II - A Phase IV Study of 3 Antiretroviral Medicines in Combination, in HIV Patients Who Have Not Been Previously Treated With Antiretroviral Therapy |
| NCT00120354 | PHASE4 | COMPLETED | Long-Term Lamivudine Therapy for Chronic Hepatitis B |
| NCT00127972 | PHASE4 | COMPLETED | 2NN & CHARM Long-Term Follow-up Study |
| NCT00143728 | PHASE4 | SUSPENDED | 3TC or No 3TC for HIV With 3TC Resistance |
| NCT00144157 | PHASE4 | COMPLETED | Open Label Study of NVP+CBV Treatment in Women Who Have Received sdNVP for the pMTCT of HIV |
| NCT00162643 | PHASE4 | UNKNOWN | PI Vs. NNRTI Based Therapy for HIV Advanced Disease |
| NCT00192621 | PHASE4 | COMPLETED | Seronegatives and Metabolic Abnormalities Protocol 2 (SAMA002): Study to Compare the Effect of Kaletra and Combivir® in HIV-Negative Healthy Subjects |
| NCT00192660 | PHASE4 | COMPLETED | HIV Infection And Metabolic Abnormalities Protocol 1 (HAMA001) |
| NCT00230477 | PHASE4 | COMPLETED | Hepsera Versus Hepsera Plus Lamivudine for Treatment of Chronic Hepatitis B in Patients With Normal ALT |
| NCT00244712 | PHASE4 | COMPLETED | Abacavir/Lamivudine Versus Emtricitabine/Tenofovir Both In Combination With Lopinavir/Ritonavir For The Treatment Of HIV |
| NCT00256828 | PHASE4 | COMPLETED | Once a Day (QD) - Twice a Day (BID) Clinical Trial: Didanosine, Lamivudine and Efavirenz Versus Zidovudine, Lamivudine and Efavirenz in the Starting Treatment of HIV |
| NCT00324649 | PHASE4 | COMPLETED | Peripheral Body Fat Distribution After Switching Zidovudine and Lamivudine to Truvada |
| NCT00337922 | PHASE4 | COMPLETED | Pharmacokinetic Study Of EPZICOM Tablet |
| NCT00342355 | PHASE4 | COMPLETED | Antiretroviral Therapy for Advanced HIV Disease in South Africa |
| NCT00354653 | PHASE4 | COMPLETED | A Trial To Study The Effect Of Lamivudine In Adult Patients Who Suffer From Chronic Hepatitis B Alone |
| NCT00380614 | PHASE4 | COMPLETED | A Randomized Controlled Trial of Lamivudine in Acute Hepatitis B |
| NCT00380770 | PHASE4 | COMPLETED | HIV/AIDS Kaposis Sarcoma: Comparison of Response to HAART vs HAART Plus CXT |
| NCT00385957 | PHASE4 | COMPLETED | Immunological and Viral Response to Antiretrovirals in HIV Patients With CD4 Cell Count Below 100 |
| NCT00393484 | PHASE4 | COMPLETED | A Study in Korea of Entecavir Versus Lamivudine in Adults With Chronic Hepatitis B Infection |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 1 clinical and 23 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).