Daclatasvir
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Also known as BMS 790052BMS-790052EBP 883EBP-883DACLATASVIR (BMS-790052)Daclatasvir dihydrochlorideÊDaclatasvir dihydrochlorideÂ
Summary
Daclatasvir (CHEMBL2023898) is an approved small-molecule nonstructural protein 5A inhibitor (ATC J05AP07); indicated across 8 conditions including viral infectious disease and hepatitis c virus infection.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: J05AP07
- Indications: 8 conditions
- Clinical trials: 101
- Chemistry: 738.9 Da · C40H50N8O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL2023898 |
| Name | Daclatasvir |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 25154714 |
| ChEBI | CHEBI:82977 |
| ATC | J05AP07 |
| Molecular formula | C40H50N8O6 |
| Molecular weight | 738.9 |
| InChIKey | FKRSSPOQAMALKA-CUPIEXAXSA-N |
SMILES: CC(C)[C@@H](C(=O)N1CCC[C@H]1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)[C@@H]6CCCN6C(=O)[C@H](C(C)C)NC(=O)OC)NC(=O)OC
IUPAC name: methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate
ChEBI definition: A member of the class of biphenyls that is a potent inhibitor of nonstructural protein 5A and is used (as its hydrochloride salt) for treatment of hepatitis C.
Pharmacological roles (ChEBI): nonstructural protein 5A inhibitor, antiviral drug.
Also known as: BMS 790052, BMS-790052, Daclatasvir, EBP 883, EBP-883, daclatasvir, DACLATASVIR, DACLATASVIR (BMS-790052), Daclatasvir dihydrochlorideÊ, Daclatasvir (BMS-790052), Daclatasvir dihydrochlorideÂ
Parent form; salt/anhydrous children: CHEMBL2303621
Patent coverage: 721 distinct patent families (1,617 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,614 (100%) 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
Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Kappa-type opioid receptor, Voltage-gated inwardly rectifying potassium channel KCNH2, Cytochrome P450 2C9, Cytochrome P450 3A4, Nuclear receptor subfamily 1 group I member 2, Bile salt export pump.
Bioactivity
ChEMBL activities: 5 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| OPRK1 | 5.39 | AC50 | 4100 | nM | CHEMBL_ACT_25129266 |
| ABCB11 | 5.23 | AC50 | 5900 | nM | CHEMBL_ACT_25126935 |
| CYP3A4 | 5.14 | IC50 | 7200 | nM | CHEMBL_ACT_10942082 |
| CYP3A4 | 5.14 | IC50 | 7200 | nM | CHEMBL_ACT_12721478 |
| CYP3A4 | 5.14 | IC50 | 7200 | nM | CHEMBL_ACT_15075589 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
8 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 C virus infection | 3 | MONDO:0005231 | EFO:0003047 |
| chronic hepatitis C virus infection | 3 | MONDO:0005354 | EFO:0004220 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | EFO:0000694 |
| hepatitis B virus infection | 2 | MONDO:0005344 | EFO:0004197 |
| chronic kidney disease | 2 | MONDO:0005300 | EFO:0003884 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 101.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 31 |
| PHASE2 | 31 |
| Not specified | 12 |
| PHASE1 | 11 |
| PHASE2/PHASE3 | 9 |
| PHASE4 | 5 |
| PHASE1/PHASE2 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02304159 | PHASE4 | COMPLETED | Study to Evaluate the Safety and Efficacy of Daclatasvir/Sofosbuvir/Ribavirin for 16 Versus 24 Weeks for HCV Genotype 3 Cirrhotics |
| NCT02624063 | PHASE4 | COMPLETED | Randomized Clinical Trial of Sofosbuvir in Combination With Daclatasvir or Simeprevir for 12 Weeks in Non-cirrhotic Subjects Infected With Chronic Hepatitis C Virus Genotype 1 (TNT) |
| NCT02992457 | PHASE4 | COMPLETED | Safety and Efficacy of Sofosbuvir-Based Regimens in the Treatment of Egyptian Patients With Hepatitis C Infection |
| NCT03200184 | PHASE4 | COMPLETED | Sofosbuvir and Daclatasvir in Treating Hepatitis C, A Study on 1000 Patients |
| NCT04457050 | PHASE4 | COMPLETED | Effect of Hepatitis C Clearance on Insulin Resistance |
| NCT01389323 | PHASE3 | COMPLETED | BMS-790052 (Daclatasvir) Plus Peg-Interferon Alfa-2a and Ribavirin in Treatment-Naive Black/African-Americans, Latinos and White/Caucasians With Hepatitis C |
| NCT01448044 | PHASE3 | COMPLETED | Phase III BMS-790052 Add-On to Peg-Interferon Alfa-2a and Ribavirin in Naive Hepatitis C |
| NCT01471574 | PHASE3 | COMPLETED | Safety and Efficacy Study of Daclatasvir (BMS-790052) Plus Pegylated Interferon-Alfa 2a and Ribavirin in Patients Coinfected With Untreated Hepatitis C Virus and HIV Virus |
| NCT01492426 | PHASE3 | COMPLETED | Study Comparing Daclatasvir (BMS-790052) With Telaprevir Combined With Peginterferon Alfa-2a and Ribavirin in Patients With Chronic Hepatitis C Virus Infection |
| NCT01497834 | PHASE3 | COMPLETED | A Phase 3 Study in Combination With BMS-790052 and BMS-650032 in Japanese Hepatitis C Virus (HCV) Patients |
| NCT01573351 | PHASE3 | COMPLETED | Phase III Hallmark QUAD: ASV+DCV+Peg+Rib (Nulls/Partials) |
| NCT01581203 | PHASE3 | COMPLETED | Phase III Hallmark DUAL: ASV+DCV (Nulls/Partials, Intolerants/Ineligibles. Naives) |
| NCT01616524 | PHASE3 | COMPLETED | Safety and Efficacy Study of Pegylated Interferon Lambda With and Without Daclatasvir, Compared to Pegylated Interferon Alfa, Plus Ribavirin in Subjects With Hepatitis C Genotype 2 and 3 |
| NCT01718145 | PHASE3 | COMPLETED | A Phase 3, Comparative Study of Asunaprevir and Daclatasvir Combination Therapy Versus Telaprevir Therapy in Japanese HCV Subjects |
| NCT01718158 | PHASE3 | COMPLETED | Efficacy and Safety Evaluation of a Regimen Consisting of Peginterferon Lambda-1a + Ribavirin + Daclatasvir (Lambda + RBV + DCV) in HCV Genotype 1b Treatment naïve Patients or Prior Relapsers to Peginterferon Alfa + Ribavirin (Alfa + RBV) Therapy |
| NCT01741545 | PHASE3 | COMPLETED | Safety and Efficacy Study in Subjects With Chronic HCV and Underlying Hemophilia |
| NCT01797848 | PHASE3 | WITHDRAWN | Efficacy and Safety Evaluation of a Treatment Consisting of Peg Interferon Alfa + Ribavirin + Daclatasvir in HCV Genotype 1 and 4 Treatment naïve Patients |
| NCT01866930 | PHASE3 | TERMINATED | Efficacy and Safety Study of Pegylated Interferon Lambda-1a With Ribavirin and Daclatasvir, to Treat naïve Subjects With Chronic HCV Genotypes 1, 2, 3, and 4 Who Are Co-infected With HIV |
| NCT01973049 | PHASE3 | COMPLETED | UNITY 2: A Study of an Investigational Treatment Regimen of DCV+ASV+BMS-791325 in a Fixed Dose Combination (the DCV 3DAA (Direct Acting Antiviral) Regimen) With or Without RBV for 12 Weeks for the Treatment of Chronic Hepatitis C Virus(HCV)Genotype 1 Infection in Subjects With Compensated Cirrhosis |
| NCT01995266 | PHASE3 | COMPLETED | Phase III China GT 1b Interferon (IFN) Intolerant Prev Exclude Dual |
| NCT02032875 | PHASE3 | COMPLETED | Phase III Daclatasvir, Sofosbuvir, and Ribavirin in Cirrhotic Participants and Participants Post-liver Transplant |
| NCT02032888 | PHASE3 | COMPLETED | A Phase 3 Study to Evaluate Combination Therapy With Daclatasvir and Sofosbuvir in the Treatment of HIV and Hepatitis C Virus Coinfection. |
| NCT02032901 | PHASE3 | COMPLETED | Phase III Daclatasvir and Sofosbuvir for Genotype 3 Chronic HCV |
| NCT02123654 | PHASE3 | COMPLETED | UNITY 3: A Japanese Phase 3 Study of a Daclatasvir/Asunaprevir/BMS-791325 in Subjects With Genotype 1 Chronic Hepatitis C |
| NCT02282709 | PHASE3 | COMPLETED | Effect of ASV and DCV Therapy on the Quality of Immune Status in Chronic HCV Patients |
| NCT02319031 | PHASE3 | COMPLETED | Safety and Efficacy Study of the Combination Daclatasvir (60 mg), Sofosbuvir (400 mg) and Ribavirin (Weight-based Dosing) for 12 or 16 Weeks in Subjects With Genotype 3 Chronic HCV Infection With or Without Prior Treatment Experience and Advanced Fibrosis or Compensated Cirrhosis |
| NCT02473211 | PHASE2/PHASE3 | COMPLETED | SOF Plus DCV in Treating Chinese Treatment-experienced HCV Patients |
| NCT02496078 | PHASE3 | COMPLETED | A Phase 3 Evaluation of Daclatasvir and Asunaprevir in Treatment-naive Subjects With Chronic Hepatitis C Genotype 1b Infection |
| NCT02555943 | PHASE2/PHASE3 | COMPLETED | DAAs Treatment for Chronic HCV/HBV Co-infection Patients(DASCO) |
| NCT02576314 | PHASE3 | COMPLETED | Sofosbuvir Containing Regimens for the Treatment of Chronic HCV GT3 Infected Patients |
| NCT02596880 | PHASE3 | COMPLETED | Sofosbuvir, Daclatasvir, Ribavirin for Hepatitis C Virus (HCV) Cirrhotics |
| NCT02640157 | PHASE3 | COMPLETED | A Study Comparing Efficacy and Safety of ABT-493/ABT-530 to Sofosbuvir Dosed With Daclatasvir in Adults With HCV Genotype 3 Infection |
| NCT02771405 | PHASE3 | COMPLETED | Impact of Interferon Free Regimens in Patients With Chronic HCV and Successfully Treated HCC |
| NCT03004625 | PHASE3 | COMPLETED | Daclatasvir, Asunaprevir Plus Ribavirin for HCV Genotype 1b Without NS5A RAV |
| NCT03163849 | PHASE3 | UNKNOWN | Assessment Effects After Direct Acting Antiviral in Chronic Hepatitis c Virus Patients |
| NCT03186313 | PHASE3 | COMPLETED | A Study to Evaluate the Safety and Efficacy of the Combined Single Dose of Dactavira Plus Or Dactavira in Egyptian Adults With Chronic Genotype 4 HCV Infection |
| NCT03369327 | PHASE3 | COMPLETED | Sofosbuvir and Daclatasvir for Treating Hepatitis C in 200 Patients Co-infected With Human Immunodeficiency Virus |
| NCT03480932 | PHASE2/PHASE3 | COMPLETED | Role of Pegylated Interferon in Combination With DAAs to Cure Hepatitis C As Soon As Possible - Hepatitis C [ASAP-C] |
| NCT03540212 | PHASE2/PHASE3 | UNKNOWN | Clinical Pharmacokinetics of Daclatasvir/Sofosbuvir in Adolescents With Hepatitis C Virus |
| NCT03883698 | PHASE3 | COMPLETED | Safety of Sofosbuvir in People With Advanced Kidney Failure |
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 10 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).