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iptacopan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| complement receptor antagonists or complement inhibitors | 5754 | 1644670-37-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Iptacopan binds to Factor B of the alternative complement pathway and regulates the cleavage of C3, generation of downstream effectors, and the amplification of the terminal pathway. In PNH, intravascular hemolysis (IVH) is mediated by the downstream membrane attack complex (MAC), while extravascular hemolysis (EVH) is facilitated by C3b opsonization. Iptacopan acts proximally in the alternative pathway of the complement cascade to control both C3b-mediated EVH and terminal complement-mediated IVH.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.252 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.133 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 5.321 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 1.652 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 36.370 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 46.210 | % | High | 1 |
| herg | hERG pIC50 | 4.699 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.413 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 3.184 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 34.990 | % | High | 1 |
| kinase-safety-class | EIF2AK3,GRK2,PDK1,PDK2,PDK4 | 5 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,PRKDC,SIK2,STK33,TEK | 13 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 3.733 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 6.266 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 5.176 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 39.070 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 7.762 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 45.810 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.039 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 3.281 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.690 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 35.940 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 885.116 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 5, 2023 | FDA | NOVARTIS PHARMS CORP |
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 |
|---|---|---|---|---|---|---|
| Breakthrough haemolysis | 93.54 | 41.32 | 11 | 303 | 230 | 90627903 |
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 |
|---|---|---|---|---|---|---|
| Breakthrough haemolysis | 63.71 | 38.70 | 8 | 237 | 173 | 42620917 |
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 |
|---|---|---|---|---|---|---|
| Breakthrough haemolysis | 90.25 | 37.07 | 11 | 421 | 276 | 110588591 |
| Pyrexia | 38.72 | 37.07 | 30 | 402 | 898235 | 109690632 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L04AJ08 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Complement inhibitors |
| FDA EPC | N0000194111 | Complement Factor B Inhibitor |
| FDA MoA | N0000194112 | Complement Factor B Inhibitors |
| CHEBI has role | CHEBI:50846 | immunomodulator |
| CHEBI has role | CHEBI:229655 | complement factor B inhibitor |
Related Drugs by ATC class:
L04AJ Complement inhibitors 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Paroxysmal nocturnal hemoglobinuria | indication | 1963002 | DOID:0060284 |
| Unresolved serious infection caused by encapsulated bacteria | contraindication |
🐶 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 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 10093663 | July 14, 2034 | TREATMENT OF COMPLEMENT 3 GLOMERULOPATHY (C3G) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 10093663 | July 14, 2034 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 11723901 | Aug. 30, 2038 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 12285422 | Aug. 30, 2038 | TREATMENT OF COMPLEMENT 3 GLOMERULOPATHY (C3G) BY ADMINISTRATION OF 200 MG OF IPTACOPAN TWICE DAILY |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 12384758 | May 17, 2041 | TREATMENT OF COMPLEMENT 3 GLOMERULOPATHY (C3G) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 12384758 | May 17, 2041 | TREATMENT OF PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 11951101 | July 15, 2041 | TREATMENT OF PAROXYSMAL NOCTURNAL HEMOGLOBINURIA (PNH) BY ADMINISTRATION OF 200 MG OF IPTACOPAN TWICE DAILY |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | 12453726 | July 15, 2041 | TREATMENT OF PAROXYSMAL NOCTURAL HEMOGLOBINURIA (PNH) BY ADMINISTRATION OF 200 MG OF IPTACOPAN TWICE DAILY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | Aug. 7, 2027 | FOR THE REDUCTION OF PROTEINURIA IN ADULTS WITH PRIMARY IMMUNOGLOBULIN A NEPHROPATHY (IGAN) AT RISK OF RAPID DISEASE PROGRESSION, GENERALLY A URINE PROTEIN-TO-CREATININE RATIO (UPCR)>/= 1.5 G/G |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | March 20, 2028 | TREATMENT OF ADULTS WITH COMPLEMENT 3 GLOMERULOPATHY (C3G), TO REDUCE PROTEINURIA |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | Dec. 5, 2028 | NEW CHEMICAL ENTITY |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | Dec. 5, 2030 | TREATMENT OF ADULTS WITH PAROXYSMAL NOCTURNAL HEMOGLOBINURIA (PNH) |
| EQ 200MG BASE | FABHALTA | NOVARTIS | N218276 | Dec. 5, 2023 | RX | CAPSULE | ORAL | March 20, 2032 | TREATMENT OF ADULTS WITH COMPLEMENT 3 GLOMERULOPATHY (C3G), TO REDUCE PROTEINURIA |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Complement factor B | Enzyme | INHIBITOR | IC50 | 8.02 | DRUG LABEL | DRUG LABEL | |||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 7.92 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| CHEBI:229652 | CHEBI |
| CHEMBL4594448 | ChEMBL_ID |
| C000730766 | MESH_SUPPLEMENTAL_RECORD_UI |
| 10710 | IUPHAR_LIGAND_ID |
| DB16200 | DRUGBANK_ID |
| 4042880 | VANDF |
| C5418258 | UMLSCUI |
| JGQ | PDB_CHEM_ID |
| CHEMBL5095401 | ChEMBL_ID |
| 11259 | INN_ID |
| 2447007-60-3 | SECONDARY_CAS_RN |
| 90467622 | PUBCHEM_CID |
| 376049 | MMSL |
| 42255 | MMSL |
| d10150 | MMSL |
| 019624 | NDDF |
| 019625 | NDDF |
| 8E05T07Z6W | UNII |
| 2671061 | RXNORM |
| D12251 | KEGG_DRUG |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| FABHALTA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0078-1189 | CAPSULE | 200 mg | ORAL | NDA | 29 sections |