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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:

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Property	Value	Reference
S (Water solubility)	700 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	3	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	13.50 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	1 mL/min/kg	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.67 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.01 %	Lombardo F, Berellini G, Obach RS

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Approvals:

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

FDA Adverse Event Reporting System (Female)

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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	327.46	30.34	62	3331	2132	63483497
Hepatitis C	199.22	30.34	48	3345	5226	63480403
Genotype drug resistance test positive	135.84	30.34	23	3370	410	63485219
Ascites	128.47	30.34	56	3337	40672	63444957
Hepatic encephalopathy	107.92	30.34	35	3358	11247	63474382
Hepatic failure	83.89	30.34	40	3353	35616	63450013
Fatigue	70.49	30.34	149	3244	887879	62597750
Headache	64.29	30.34	118	3275	633123	62852506
Oesophageal varices haemorrhage	61.11	30.34	14	3379	1220	63484409
Hepatic cirrhosis	58.92	30.34	28	3365	24706	63460923

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FDA Adverse Event Reporting System (Male)

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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	988.48	24.78	234	5780	7275	34943642
Hepatitis C	692.81	24.78	186	5828	9644	34941273
Genotype drug resistance test positive	683.12	24.78	125	5889	1020	34949897
Treatment failure	486.79	24.78	210	5804	46487	34904430
Liver transplant	211.75	24.78	55	5959	2479	34948438
Viral mutation identified	148.50	24.78	43	5971	2911	34948006
Hepatic encephalopathy	139.24	24.78	62	5952	14623	34936294
Drug ineffective	112.21	24.78	243	5771	456508	34494409
Hepatic cirrhosis	105.66	24.78	54	5960	17260	34933657
Fatigue	104.66	24.78	209	5805	370444	34580473

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FDA Adverse Event Reporting System (Geriatric)

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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	1194.09	24.67	259	8280	8762	79727087
Hepatitis C	768.89	24.67	191	8348	11734	79724115
Genotype drug resistance test positive	571.00	24.67	102	8437	1206	79734643
Hepatic encephalopathy	243.18	24.67	93	8446	24073	79711776
Liver transplant	240.92	24.67	62	8477	4361	79731488
Treatment failure	237.99	24.67	174	8365	170312	79565537
Ascites	215.15	24.67	121	8418	75441	79660408
Viral mutation identified	200.00	24.67	52	8487	3806	79732043
Fatigue	147.82	24.67	313	8226	929414	78806435
Hepatic failure	137.16	24.67	84	8455	61128	79674721

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:83799	nonstructural protein 5A inhibitors
FDA EPC	N0000191256	Hepatitis C Virus NS5A Inhibitor
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

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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

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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

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Orange Book patent data (new drug applications)

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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 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 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	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

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Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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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

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External reference:

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ID	Source
015679	NDDF
1009119-65-6	SECONDARY_CAS_RN
11266	IUPHAR_LIGAND_ID
1172356004	SNOMEDCT_US
1606217	RXNORM
229788	MMSL
25154714	PUBCHEM_CID
30519	MMSL
4034682	VUID
4034682	VANDF

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Pharmaceutical products:

None