All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

difelikefalin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
enkephalin, endorphin and dynorphin opioid delta, miu and kappa receptor agonists	5470	1024828-77-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: difelikefalin difelikefalin acetate korsuva CR845 FE202845 MR13A9 kapruvia	Difelikefalin is a kappa opioid receptor (KOR) agonist. The relevance of KOR activation to therapeutic effectiveness is not known. Molecular weight: 679.86 Formula: C36H53N7O6 CLOGP: 0.63 LIPINSKI: 3 HAC: 13 HDO: 7 TPSA: 222.97 ALOGS: -4.82 ROTB: 18 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
15	mcg	P

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AKT3,AXL,BRAF,BTK,CAMK2D,CDK5,EIF2AK3,ERBB2,GRK2,ITK,JAK3,MAPK10,MAPK7,MET,NTRK2,PDK2,PDK4,PIK3CA,PRKDC,TEK,TGFBR1	22
kinase-selectivity-class	GRK2,PDK4	2
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Aug. 23, 2021	FDA	CARA THERAPEUTICS INC
April 25, 2022	EMA	VIFOR FRESENIUS MEDICAL CARE RENAL PHARMA FRANCE

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
Drug reaction with eosinophilia and systemic symptoms	66.47	52.16	14	88	42744	90585601
Somnolence	53.04	52.16	16	86	209068	90419277

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	V03AX04	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Other therapeutic products
FDA EPC	N0000194001	Kappa Opioid Receptor Agonist
FDA MoA	N0000194007	Opioid kappa Receptor Agonists
CHEBI has role	CHEBI:35480	analgesic

Related Drugs by ATC class:

V03AX Other therapeutic products 2 drugs

cobicistatnalfurafine

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

Disease	Relation	SNOMED_ID	DOID
Pruritus associated with chronic kidney disease (CKD-aP)	indication	707151000

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	10017536	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	10138270	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	10793596	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	7713937	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	7727963	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	8217007	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	8236766	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	8486894	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	8536131	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	9334305	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	9359399	Nov. 12, 2027	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	7402564	Nov. 12, 2032	TREATMENT OF MODERATE-TO-SEVERE PRURITUS ASSOCIATED WITH CHRONIC KIDNEY DISEASE (CKD-AP) IN ADULTS UNDERGOING HEMODIALYSIS (HD)

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 0.065MG BASE/1.3ML (EQ 0.05MG BASE/ML)	KORSUVA	VIFOR INTL	N214916	Aug. 23, 2021	RX	SOLUTION	INTRAVENOUS	Aug. 23, 2026	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	AGONIST	Ki	9.49		DRUG LABEL
Kappa-type opioid receptor	GPCR		OPRK_MOUSE	AGONIST	EC50	10.32		IUPHAR

External reference:

ID	Source
NA1U919MRO	UNII
1024829-44-4	SECONDARY_CAS_RN
C4519744	UMLSCUI
CHEBI:756409	CHEBI
CHEMBL3989915	ChEMBL_ID
24794466	PUBCHEM_CID
DB11938	DRUGBANK_ID
CHEMBL5315123	ChEMBL_ID
D11111	KEGG_DRUG
10179	INN_ID
C000657129	MESH_SUPPLEMENTAL_RECORD_UI
9044	IUPHAR_LIGAND_ID
40963111000001109	SNOMEDCT_US
40963211000001103	SNOMEDCT_US
4041254	VANDF
349719	MMSL
39827	MMSL
d09794	MMSL
018837	NDDF
018838	NDDF
2569089	RXNORM
NA1U919MRO	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Korsuva	HUMAN PRESCRIPTION DRUG LABEL	1	59353-065	INJECTION, SOLUTION	50 ug	INTRAVENOUS	NDA	27 sections