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copanlisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| phosphatidylinositol 3-kinase inhibitors, antineoplastics | 5256 | 1032568-63-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Copanlisib is an inhibitor of phosphatidylinositol-3-kinase (PI3K) with inhibitory activity predominantly against PI3K-alpha and PI3K-delta isoforms expressed in malignant B cells. Copanlisib has been shown to induce tumor cell death by apoptosis and inhibition of proliferation of primary malignant B cell lines. Copanlisib inhibits several key cell-signaling pathways, including B-cell receptor (BCR) signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFkB signaling in lymphoma cell lines.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 6.43 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 10.34 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 6.42 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 25.20 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.853 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 44.361 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 2.618 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.846 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 32.980 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 40.230 | % | High | 1 |
| herg | hERG pIC50 | 4.612 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.245 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 19.364 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 23.190 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK9,CSF1R,DDR1,FLT3,GRK2,ITK,MAP3K21,MAPK7,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,SIK2 | 20 | |||
| kinase-selectivity-class | ACVR2B,AXL,BRAF,FLT3,MAP3K21,MAPK7,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,SIK2 | 12 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 18.323 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 8.222 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 26.230 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 23.442 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 45.520 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 4.613 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 60.110 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 21.560 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 10.069 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 14, 2017 | FDA | BAYER HEALTHCARE PHARMS |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Metastases to muscle | 66.66 | 52.09 | 9 | 573 | 376 | 110588341 |
| Metastases to retroperitoneum | 65.71 | 52.09 | 9 | 573 | 419 | 110588298 |
| Cytopenia | 62.88 | 52.09 | 17 | 565 | 30099 | 110558618 |
| Pyrexia | 62.57 | 52.09 | 45 | 537 | 898220 | 109690497 |
| Neutropenic sepsis | 62.54 | 52.09 | 17 | 565 | 30729 | 110557988 |
| Metastases to spleen | 59.60 | 52.09 | 9 | 573 | 835 | 110587882 |
| Metastases to bone marrow | 57.95 | 52.09 | 9 | 573 | 1005 | 110587712 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EM02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Phosphatidylinositol-3-kinase (Pi3K) inhibitors |
| FDA MoA | N0000175082 | Kinase Inhibitors |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50914 | EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor |
| CHEBI has role | CHEBI:68495 | apoptosis inducer |
Related Drugs by ATC class:
L01EM Phosphatidylinositol-3-kinase (Pi3K) inhibitors 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Follicular lymphoma | indication | 55150002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.78 | acidic |
| pKa2 | 9.17 | Basic |
| pKa3 | 7.65 | Basic |
| pKa4 | 6.36 | Basic |
| pKa5 | 2.69 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | Kinase | INHIBITOR | IC50 | 9.16 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Kinase | INHIBITOR | IC50 | 9.30 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Serine/threonine-protein kinase mTOR | Kinase | INHIBITOR | IC50 | 7.35 | IUPHAR | ||||
| Ras-related protein Rab-27A | Enzyme | Kd | 5.35 | CHEMBL | |||||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | Kinase | INHIBITOR | IC50 | 8.43 | SCIENTIFIC LITERATURE | ||||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Kinase | INHIBITOR | IC50 | 8.19 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| WI6V529FZ9 | UNII |
| 1402152-13-9 | SECONDARY_CAS_RN |
| 1402152-46-8 | SECONDARY_CAS_RN |
| 4036879 | VANDF |
| C4049141 | UMLSCUI |
| CHEBI:173077 | CHEBI |
| CHEMBL3218576 | ChEMBL_ID |
| 135565596 | PUBCHEM_CID |
| DB12483 | DRUGBANK_ID |
| CHEMBL3545068 | ChEMBL_ID |
| D10797 | KEGG_DRUG |
| 9726 | INN_ID |
| C000589253 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7875 | IUPHAR_LIGAND_ID |
| 741057007 | SNOMEDCT_US |
| 763592006 | SNOMEDCT_US |
| 6E2 | PDB_CHEM_ID |
| d08659 | MMSL |
| 017343 | NDDF |
| 1945077 | RXNORM |
| WI6V529FZ9 | INXIGHT DRUGS |
Pharmaceutical products:
None