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

Stem definition	Drug id	CAS RN
	5155	459789-99-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: obeticholic acid ocaliva 6-ECDCA 6ECDCA INT-747	obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine Molecular weight: 420.63 Formula: C26H44O4 CLOGP: 5.36 LIPINSKI: 1 HAC: 4 HDO: 3 TPSA: 77.76 ALOGS: -4.58 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

obeticholic acid
ocaliva
6-ECDCA
6ECDCA
INT-747

obeticholic acid is an agonist for FXR, a nuclear receptor expressed in the liver and intestine

Molecular weight: 420.63
Formula: C26H44O4
CLOGP: 5.36
LIPINSKI: 1
HAC: 4
HDO: 3
TPSA: 77.76
ALOGS: -4.58
ROTB: 5

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 12, 2016	EMA	Intercept Pharma Ltd
May 27, 2016	FDA	INTERCEPT PHARMACEUTICALS INC

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
Pruritus	1505.08	29.80	657	4128	360796	63123441
Therapy cessation	247.00	29.80	91	4694	30366	63453871
Hospitalisation	210.19	29.80	110	4675	84971	63399266
Therapy interrupted	171.08	29.80	71	4714	32384	63451853
Product dose omission issue	160.77	29.80	136	4649	234177	63250060
Blood alkaline phosphatase abnormal	140.89	29.80	26	4759	539	63483698
Hepatic cirrhosis	103.54	29.80	46	4739	24688	63459549
Blood alkaline phosphatase increased	93.07	29.80	51	4734	42916	63441321
Fatigue	92.30	29.80	204	4581	887824	62596413
Hepatic fibrosis	83.57	29.80	24	4761	3628	63480609

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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
Pruritus	163.29	42.26	57	272	141924	34814678
Hospitalisation	42.74	42.26	17	312	56885	34899717

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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
Pruritus	1312.09	30.20	529	3129	394119	79346611
Therapy cessation	180.57	30.20	67	3591	37495	79703235
Product dose omission issue	127.80	30.20	99	3559	247438	79493292
Therapy interrupted	108.22	30.20	44	3614	31297	79709433
Fatigue	89.43	30.20	155	3503	929572	78811158
Blood alkaline phosphatase abnormal	85.77	30.20	17	3641	865	79739865
Hepatic cirrhosis	84.12	30.20	38	3620	34868	79705862
Blood alkaline phosphatase increased	75.79	30.20	43	3615	63621	79677109
Hospitalisation	72.14	30.20	48	3610	94188	79646542
Insurance issue	50.03	30.20	16	3642	5717	79735013

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A05AA04	ALIMENTARY TRACT AND METABOLISM BILE AND LIVER THERAPY BILE THERAPY Bile acids and derivatives
CHEBI has role	CHEBI:62868	hepatoprotective agents
CHEBI has role	CHEBI:132972	farnesoid X receptor agonists
FDA EPC	N0000192561	Farnesoid X Receptor Agonist
FDA MoA	N0000192560	Farnesoid X Receptor Agonists

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

Disease	Relation	SNOMED_ID	DOID
Primary cholangitis	indication	17266006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.92	acidic

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
10MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	10047117	Sept. 6, 2033	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC)
10MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	10758549	April 26, 2036	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC) IN COMBINATION WITH URSODEOXYCHOLIC ACID (UDCA) IN ADULTS WITH AN INADEQUATE RESPONSE TO UDCA, OR AS MONOTHERAPY IN ADULTS UNABLE TO TOLERATE UDCA
5MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	10047117	Sept. 6, 2033	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC)
5MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	10758549	April 26, 2036	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC) IN COMBINATION WITH URSODEOXYCHOLIC ACID (UDCA) IN ADULTS WITH AN INADEQUATE RESPONSE TO UDCA, OR AS MONOTHERAPY IN ADULTS UNABLE TO TOLERATE UDCA

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	May 27, 2023	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC) IN COMBINATION WITH URSODEOXYCHOLIC ACID (UDCA) IN ADULTS WITH AN INADEQUATE RESPONSE TO UDCA, OR AS MONOTHERAPY IN ADULTS UNABLE TO TOLERATE UDCA
5MG	OCALIVA	INTERCEPT PHARMS INC	N207999	May 27, 2016	RX	TABLET	ORAL	May 27, 2023	TREATMENT OF PRIMARY BILIARY CHOLANGITIS (PBC) IN COMBINATION WITH URSODEOXYCHOLIC ACID (UDCA) IN ADULTS WITH AN INADEQUATE RESPONSE TO UDCA, OR AS MONOTHERAPY IN ADULTS UNABLE TO TOLERATE UDCA

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN	AGONIST	EC50	7.00		SCIENTIFIC LITERATURE	DRUG LABEL
G-protein coupled bile acid receptor 1	GPCR	Q8TDU6	GPBAR_HUMAN		EC50	7		CHEMBL

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External reference:

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ID	Source
016875	NDDF
0462Z4S4OZ	UNII
1798288	RXNORM
241391	MMSL
31698	MMSL
3435	IUPHAR_LIGAND_ID
4035786	VANDF
447715	PUBCHEM_CID
720257002	SNOMEDCT_US
763557003	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-005	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-005	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-005	TABLET, FILM COATED	5 mg	ORAL	NDA	32 sections
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-010	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-010	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections
Ocaliva	HUMAN PRESCRIPTION DRUG LABEL	1	69516-010	TABLET, FILM COATED	10 mg	ORAL	NDA	32 sections

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