umbralisib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
phosphatidylinositol 3-kinase inhibitors, antineoplastics	5441	1532533-67-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: umbralisib umbralisib tosylate ukoniq TGR-1202	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. Molecular weight: 571.56 Formula: C31H24F3N5O3 CLOGP: 5.83 LIPINSKI: 2 HAC: 8 HDO: 1 TPSA: 105.15 ALOGS: -5.53 ROTB: 6 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

umbralisib
umbralisib tosylate
ukoniq
TGR-1202

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.

Molecular weight: 571.56
Formula: C31H24F3N5O3
CLOGP: 5.83
LIPINSKI: 2
HAC: 8
HDO: 1
TPSA: 105.15
ALOGS: -5.53
ROTB: 6

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

None

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	50.48	43.87	10	52	14533	34942336

FDA Adverse Event Reporting System (Geriatric)

None

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
FDA MoA	N0000175082	Kinase Inhibitors
FDA EPC	N0000175605	Kinase Inhibitor

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])	Bioact source	MoA source
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	Kinase	O00329	PK3CD_HUMAN	INHIBITOR	Kd	8.21	SCIENTIFIC LITERATURE	DRUG LABEL
Casein kinase I isoform epsilon	Kinase	P49674	KC1E_HUMAN	INHIBITOR	Kd	6.74	SCIENTIFIC LITERATURE	DRUG LABEL
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	Kinase	P42336	PK3CA_HUMAN	INHIBITOR	Kd	5	SCIENTIFIC LITERATURE
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	Kinase	P42338	PK3CB_HUMAN	INHIBITOR	Kd	5	SCIENTIFIC LITERATURE
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Kinase	P48736	PK3CG_HUMAN	INHIBITOR	Kd	5.85	SCIENTIFIC LITERATURE

External reference:

ID	Source
D11322	KEGG_DRUG
38073MQB2A	UNII
1532533-72-4	SECONDARY_CAS_RN
C4682392	UMLSCUI
CHEMBL3948730	ChEMBL_ID
72950888	PUBCHEM_CID
DB14989	DRUGBANK_ID
CHEMBL3989869	ChEMBL_ID
8916	IUPHAR_LIGAND_ID
018630	NDDF
018631	NDDF
1148656009	SNOMEDCT_US
1148709002	SNOMEDCT_US
1148712004	SNOMEDCT_US
4040064	VANDF
2478438	RXNORM
343527	MMSL
39321	MMSL
d09711	MMSL
C000626319	MESH_SUPPLEMENTAL_RECORD_UI
10350	INN_ID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
UKONIQ	HUMAN PRESCRIPTION DRUG LABEL	1	73150-200	TABLET, FILM COATED	260.20 mg	ORAL	NDA	26 sections