difelikefalin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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 |
|---|---|
|
Synonyms:
|
Difelikefalin is a kappa opioid receptor (KOR) agonist. The relevance of KOR activation to therapeutic effectiveness is not known.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 25, 2022 | EMA | VIFOR FRESENIUS MEDICAL CARE RENAL PHARMA FRANCE | |
| Aug. 23, 2021 | FDA | CARA THERAPEUTICS INC |
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 | 77.46 | 68.66 | 13 | 17 | 33823 | 63455169 |
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 |
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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | N214916 | Aug. 23, 2021 | RX | SOLUTION | INTRAVENOUS | 7402564 | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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 | CARA THERAP | 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) |
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 | CARA THERAP | 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 | AGONIST | Ki | 9.49 | DRUG LABEL | ||||
| Kappa-type opioid receptor | GPCR | AGONIST | EC50 | 10.32 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| NA1U919MRO | UNII |
| 1024829-44-4 | SECONDARY_CAS_RN |
| C4519744 | UMLSCUI |
| CHEMBL3989915 | ChEMBL_ID |
| 24794466 | PUBCHEM_CID |
| DB11938 | DRUGBANK_ID |
| D11111 | KEGG_DRUG |
| 10179 | INN_ID |
| 9044 | IUPHAR_LIGAND_ID |
| 018837 | NDDF |
| 018838 | NDDF |
| 4041254 | VANDF |
| 2569089 | RXNORM |
| 349719 | MMSL |
| 39827 | MMSL |
| d09794 | MMSL |
| C000657129 | MESH_SUPPLEMENTAL_RECORD_UI |
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 | 25 sections |