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daclatasvir 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antivirals, hepatitis C Virus (HCV) NS5A inhibitors	4875	1009119-64-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: daclatasvir daclatasvir dihydrochloride daclatasvir hydrochloride daklinza BMS-790052-05 BMS-790052 daclatasvir HCl daclatasivr	an HCV NS5A inhibitor Molecular weight: 738.89 Formula: C40H50N8O6 CLOGP: 4.72 LIPINSKI: 2 HAC: 14 HDO: 4 TPSA: 174.64 ALOGS: -4.94 ROTB: 13 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

daclatasvir
daclatasvir dihydrochloride
daclatasvir hydrochloride
daklinza
BMS-790052-05
BMS-790052
daclatasvir HCl
daclatasivr

an HCV NS5A inhibitor

Molecular weight: 738.89
Formula: C40H50N8O6
CLOGP: 4.72
LIPINSKI: 2
HAC: 14
HDO: 4
TPSA: 174.64
ALOGS: -4.94
ROTB: 13

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
60	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	4	Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution)	0.67 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	13.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
June 27, 2014	EMA
July 24, 2015	FDA	BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatocellular carcinoma	313.90	30.33	61	3285	1938	50599840
Hepatitis C	172.55	30.33	44	3302	4873	50596905
Genotype drug resistance test positive	140.16	30.33	23	3323	267	50601511
Ascites	123.88	30.33	56	3290	35805	50565973
Hepatic encephalopathy	106.03	30.33	35	3311	9601	50592177
Hepatic failure	79.58	30.33	40	3306	32243	50569535
Fatigue	71.98	30.33	149	3197	707452	49894326
Headache	65.19	30.33	118	3228	506417	50095361
Hepatic cirrhosis	62.36	30.33	28	3318	17549	50584229
Oesophageal varices haemorrhage	60.66	30.33	14	3332	1016	50600762
Liver transplant	55.18	30.33	15	3331	2117	50599661
Hepatitis B reactivation	50.84	30.33	14	3332	2073	50599705
Viral mutation identified	44.69	30.33	12	3334	1617	50600161
Renal impairment	42.19	30.33	37	3309	75624	50526154
Liver injury	42.11	30.33	24	3322	24782	50576996
Jaundice	38.09	30.33	23	3323	26406	50575372
Treatment failure	37.84	30.33	46	3300	137591	50464187
Hepatitis B DNA increased	31.66	30.33	6	3340	165	50601613
Virologic failure	31.31	30.33	9	3337	1555	50600223
Drug resistance	31.23	30.33	18	3328	18971	50582807

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatocellular carcinoma	951.41	24.57	231	5728	6807	29561761
Genotype drug resistance test positive	677.47	24.57	125	5834	898	29567670
Hepatitis C	644.63	24.57	178	5781	8732	29559836
Treatment failure	488.84	24.57	206	5753	36733	29531835
Liver transplant	208.04	24.57	55	5904	2261	29566307
Viral mutation identified	149.08	24.57	43	5916	2445	29566123
Hepatic encephalopathy	136.94	24.57	62	5897	12973	29555595
Drug ineffective	121.85	24.57	241	5718	362929	29205639
Ascites	109.02	24.57	76	5883	36543	29532025
Fatigue	104.51	24.57	209	5750	316612	29251956
Headache	98.38	24.57	146	5813	173861	29394707
Hepatic cirrhosis	98.15	24.57	51	5908	14393	29554175
Hepatic failure	76.88	24.57	58	5901	31454	29537114
Hepatic cancer	75.09	24.57	33	5926	6423	29562145
Virologic failure	73.79	24.57	26	5933	2821	29565747
Therapeutic embolisation	73.18	24.57	16	5943	287	29568281
Hyperbilirubinaemia	66.61	24.57	40	5919	14894	29553674
Hepatitis B reactivation	59.70	24.57	23	5936	3206	29565362
Insomnia	56.56	24.57	79	5880	88682	29479886
Genital herpes simplex	49.56	24.57	10	5949	119	29568449
Biliary colic	47.16	24.57	14	5945	879	29567689
Varices oesophageal	46.27	24.57	19	5940	3127	29565441
Oesophageal varices haemorrhage	42.07	24.57	17	5942	2685	29565883
Hepatitis C RNA increased	41.70	24.57	10	5949	274	29568294
Abdominal cavity drainage	39.77	24.57	10	5949	335	29568233
Genital herpes	39.48	24.57	11	5948	550	29568018
Hepatorenal syndrome	37.60	24.57	15	5944	2291	29566277
Hepatitis C RNA positive	35.62	24.57	8	5951	163	29568405
Jaundice	33.27	24.57	35	5924	29261	29539307
Peritonitis bacterial	29.83	24.57	17	5942	5739	29562829
Embolism	29.52	24.57	18	5941	6878	29561690
Hepatic neoplasm	26.70	24.57	11	5948	1825	29566743
Hydrocholecystis	26.40	24.57	7	5952	290	29568278
Transcatheter arterial chemoembolisation	26.38	24.57	4	5955	6	29568562
Liver disorder	26.04	24.57	30	5929	27719	29540849

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Hepatocellular carcinoma	1138.65	24.56	255	8189	8148	64482140
Hepatitis C	687.34	24.56	179	8265	10836	64479452
Genotype drug resistance test positive	573.49	24.56	102	8342	942	64489346
Treatment failure	261.01	24.56	172	8272	116644	64373644
Hepatic encephalopathy	237.43	24.56	93	8351	20973	64469315
Liver transplant	233.34	24.56	62	8382	4030	64486258
Ascites	214.80	24.56	121	8323	61880	64428408
Viral mutation identified	196.98	24.56	52	8392	3294	64486994
Fatigue	151.21	24.56	313	8131	748417	63741871
Hepatic failure	124.47	24.56	82	8362	55312	64434976
Headache	124.12	24.56	236	8208	529231	63961057
Hepatic cirrhosis	123.78	24.56	63	8381	26235	64464053
Hyperbilirubinaemia	94.57	24.56	49	8395	21156	64469132
Hepatic cancer	91.36	24.56	35	8409	7413	64482875
Hepatitis B reactivation	89.98	24.56	31	8413	4858	64485430
Therapeutic embolisation	89.96	24.56	19	8425	452	64489836
Oesophageal varices haemorrhage	74.59	24.56	25	8419	3604	64486684
Virologic failure	71.72	24.56	24	8420	3442	64486846
Hepatitis C RNA increased	69.93	24.56	15	8429	385	64489903
Insomnia	68.24	24.56	105	8339	197731	64292557
Renal impairment	58.69	24.56	80	8364	134937	64355351
Varices oesophageal	55.46	24.56	22	8422	5108	64485180
Jaundice	53.52	24.56	47	8397	48465	64441823
Drug ineffective	51.27	24.56	231	8213	840016	63650272
Abdominal cavity drainage	50.96	24.56	13	8431	718	64489570
Hepatitis B DNA increased	47.85	24.56	12	8432	618	64489670
Hepatorenal syndrome	47.36	24.56	18	8426	3728	64486560
Genital herpes simplex	45.08	24.56	10	8434	301	64489987
Liver disorder	42.21	24.56	43	8401	53308	64436980
Hepatectomy	38.39	24.56	8	8436	178	64490110
Peritonitis bacterial	34.94	24.56	19	8425	9024	64481264
Biliary colic	34.56	24.56	14	8430	3430	64486858
Hydrocholecystis	33.30	24.56	8	8436	344	64489944
Genital herpes	30.97	24.56	11	8433	1884	64488404
Mesenteric vein thrombosis	30.90	24.56	10	8434	1292	64488996
Hepatitis C RNA positive	30.76	24.56	7	8437	237	64490051
Liver transplant rejection	29.44	24.56	12	8432	2987	64487301
Toxicity to various agents	29.27	24.56	6	8438	363507	64126781
Hepatic neoplasm	29.14	24.56	12	8432	3065	64487223
Acute leukaemia	28.89	24.56	10	8434	1588	64488700
Incorrect product administration duration	28.29	24.56	17	8427	9741	64480547
Portal hypertensive gastropathy	27.80	24.56	9	8435	1163	64489125
Embolism	27.16	24.56	18	8426	12217	64478071
Renal disorder	27.05	24.56	28	8416	35337	64454951
Anaemia	26.66	24.56	109	8335	378571	64111717
Transcatheter arterial chemoembolisation	25.33	24.56	4	8440	16	64490272

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	J05AP07	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections
ATC	J05AP58	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Antivirals for treatment of HCV infections
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190107	Organic Anion Transporting Polypeptide 1B1 Inhibitors
FDA MoA	N0000190108	Organic Anion Transporting Polypeptide 1B3 Inhibitors
FDA MoA	N0000190113	Breast Cancer Resistance Protein Inhibitors
FDA EPC	N0000191256	Hepatitis C Virus NS5A Inhibitor
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:83799	nonstructural protein 5A inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Chronic hepatitis C	indication	128302006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.05	acidic
pKa2	12.44	acidic
pKa3	12.88	acidic
pKa4	13.27	acidic
pKa5	6.51	Basic
pKa6	5.91	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8900566	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8900566	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8900566	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8900566	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 90MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	April 13, 2016	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 90MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	April 13, 2016	DISCN	TABLET	ORAL	9421192	Aug. 8, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8642025	Aug. 11, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8642025	Aug. 11, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8642025	Aug. 11, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8642025	Aug. 11, 2027	METHOD OF INHIBITING HEPATITIS C VIRUS WITH DAKLINZA AND AT LEAST ONE ADDITIONAL COMPOUND HAVING ANTI-HCV ACTIVITY
EQ 30MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8629171	June 13, 2031	METHOD OF INHIBITING HEPATITIS C VIRUS
EQ 60MG BASE	DAKLINZA	BRISTOL-MYERS SQUIBB	N206843	July 24, 2015	DISCN	TABLET	ORAL	8629171	June 13, 2031	METHOD OF INHIBITING HEPATITIS C VIRUS

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.53	CHEMBL
Genome polyprotein	Polyprotein		POLG_HCVBK	INHIBITOR	EC50	11.05	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Genome polyprotein	Polyprotein		POLG_HCVH	INHIBITOR	EC50	10.30	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Nonstructural protein 5A	Unclassified		Q5L478_9HEPC		IC50	10.64	CHEMBL

External reference:

ID	Source
D10065	KEGG_DRUG
4034682	VUID
N0000191739	NUI
1009119-65-6	SECONDARY_CAS_RN
4034682	VANDF
CHEBI:83800	CHEBI
CHEMBL2023898	ChEMBL_ID
C549273	MESH_SUPPLEMENTAL_RECORD_UI
11266	IUPHAR_LIGAND_ID
9483	INN_ID
DB09102	DRUGBANK_ID
LI2427F9CI	UNII
25154714	PUBCHEM_CID
1606217	RXNORM
229788	MMSL
30519	MMSL
d08285	MMSL
015679	NDDF
1172356004	SNOMEDCT_US
712519008	SNOMEDCT_US
714014007	SNOMEDCT_US
C3252090	UMLSCUI
CHEMBL2303621	ChEMBL_ID

Pharmaceutical products:

None