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umbralisib 🐶 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 | 5441 | 1532533-67-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Umbralisib inhibits multiple kinases. In biochemical and cell-based assays, umbralisib inhibited PI3Kdelta and casein kinase CK1-epsilon. PI3K-delta is expressed in normal and malignant B-cells; CK1-epsilon has been implicated in the pathogenesis of cancer cells, including lymphoid malignancies. Umbralisib also inhibited a mutated form of ABL1 in biochemical assays. Umbralisib inhibited cell proliferation, CXCL12-mediated cell adhesion, and CCL19-mediated cell migration in lymphoma cell lines in studies conducted in vitro.
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 | 4.483 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.045 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 21.577 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 9.528 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.590 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.370 | % | High | 1 |
| herg | hERG pIC50 | 4.955 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 7.047 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 10.447 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.460 | % | High | 1 |
| kinase-safety-class | ABL1,ABL2,ACVR1B,ACVR2A,ACVR2B,ACVRL1,ALK,AURKA,AURKB,AURKC,AXL,BLK,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK9,CSF1R,CSK,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB1,EPHB4,ERBB2,ERBB4,FGFR1,FLT3,FYN,GAK,GRK2,IRAK1,IRAK3,IRAK4,ITK,JAK1,KDR,KIT,LCK,LYN,MAP2K1,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK7,MARK4,MELK,MET,MINK1,MKNK2,MST1R,NTRK1,PDGFRB,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKCD,PRKDC,PTK6,RET,RIPK3,SIK2,SIK3,SRC,STK10,STK33,SYK,TGFBR1,TNIK,TTK,TYRO3,ULK1,YES1 | 85 | |||
| kinase-selectivity-class | ACVR2B,AURKA,AURKB,AXL,BRAF,CAMK2D,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,MAP3K21,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKDC,SIK2,SIK3,TGFBR1 | 22 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.354 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 31.550 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 0.540 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 1.507 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 1.050 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 37.497 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 4.280 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.590 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 2.786 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 5, 2021 | FDA | TG THERAPEUTICS Inc |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Nervous system disorder | 57.90 | 50.49 | 13 | 132 | 17182 | 42604008 |
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 |
|---|---|---|---|---|---|---|
| Nervous system disorder | 60.01 | 57.07 | 13 | 159 | 31708 | 110557419 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01EX25 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS PROTEIN KINASE INHIBITORS Other protein kinase inhibitors |
| MeSH PA | D000081082 | Phosphoinositide-3 Kinase Inhibitors |
| MeSH PA | D004791 | Enzyme Inhibitors |
| FDA MoA | N0000175082 | Kinase Inhibitors |
| FDA EPC | N0000175605 | Kinase Inhibitor |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:233423 | antifibrotic agent |
Related Drugs by ATC class:
L01EX Other protein kinase inhibitors 21 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Relapsed or refractory follicular lymphoma | indication | 55150002 | |
| Relapsed or refractory marginal zone lymphoma | indication | 447100004 |
🐶 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 | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10072013 | July 2, 2033 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10072013 | July 2, 2033 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10570142 | July 2, 2033 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10570142 | July 2, 2033 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10981919 | July 2, 2033 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10981919 | July 2, 2033 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 9669033 | July 2, 2033 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 9669033 | July 2, 2033 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10414773 | May 26, 2035 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10414773 | May 26, 2035 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10947244 | May 26, 2035 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 10947244 | May 26, 2035 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 9969740 | May 26, 2035 | RELAPSED OR REFRACTORY FOLLICULAR LYMPHOMA (FL) WHO HAVE RECEIVED AT LEAST THREE PRIOR LINES OF SYSTEMIC THERAPY |
| EQ 200MG BASE | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | 9969740 | May 26, 2035 | RELAPSED OR REFRACTORY MARGINAL ZONE LYMPHOMA (MZL) WHO HAVE RECEIVED AT LEAST ONE PRIOR ANTI-CD20-BASED REGIMEN |
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 | UKONIQ | TG THERAPS | N213176 | Feb. 5, 2021 | DISCN | TABLET | ORAL | Feb. 5, 2026 | NEW CHEMICAL ENTITY |
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 | Kd | 8.21 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Casein kinase I isoform epsilon | Kinase | INHIBITOR | Kd | 6.74 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | Kinase | INHIBITOR | Kd | 5 | SCIENTIFIC LITERATURE | ||||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | Kinase | INHIBITOR | Kd | 5 | SCIENTIFIC LITERATURE | ||||
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Kinase | INHIBITOR | Kd | 5.85 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D11322 | KEGG_DRUG |
| 38073MQB2A | UNII |
| 1532533-72-4 | SECONDARY_CAS_RN |
| C4682392 | UMLSCUI |
| CHEBI:756005 | CHEBI |
| CHEMBL3948730 | ChEMBL_ID |
| 72950888 | PUBCHEM_CID |
| DB14989 | DRUGBANK_ID |
| CHEMBL3989869 | ChEMBL_ID |
| 10350 | INN_ID |
| C000626319 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8916 | IUPHAR_LIGAND_ID |
| 1148656009 | SNOMEDCT_US |
| 1148709002 | SNOMEDCT_US |
| 1148712004 | SNOMEDCT_US |
| 4040064 | VANDF |
| 343527 | MMSL |
| 39321 | MMSL |
| d09711 | MMSL |
| 018630 | NDDF |
| 018631 | NDDF |
| 2478438 | RXNORM |
| 38073MQB2A | INXIGHT DRUGS |
Pharmaceutical products:
None