Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMYRBO1)

• Drug Name: Umbralisib Drug Info
• Synonyms: RP5264; TGR-1202

Indication

Disease Entry	ICD 11	Status	REF
Follicular lymphoma	2A80	Approved	[1]
Marginal zone lymphoma	2A85.0	Approved	[1]
Diffuse large B-cell lymphoma	2A81	Phase 2/3	[2]
Chronic lymphocytic leukaemia	2A82.0	Phase 2	[3]
Non-hodgkin lymphoma	2B33.5	Phase 2	[3]

• Cross-matching ID:
  PubChem CID: 72950888
  CAS Number: CAS 1532533-67-7
  TTD Drug ID: DMYRBO1

Molecule-Related Drug Atlas

Drug(s) Targeting PI3-kinase delta (PIK3CD)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAY 80-6946	DMLOS5R	Follicular lymphoma	2A80	Approved	[4]
Idelalisib	DM602WT	Chronic lymphocytic leukaemia	2A82.0	Approved	[5]
IPI-145	DMWA24P	Follicular lymphoma	2A80	Approved	[6]
Leniolisib	DMWAD93	Stomach cancer	2B72	Approved	[7]
Buparlisib	DM1WEHC	Breast cancer	2C60-2C65	Phase 3	[8]
INCB50465	DMZJP2T	Diffuse large B-cell lymphoma	2A81	Phase 2	[3]
ME-401	DMK0UOY	Follicular lymphoma	2A80	Phase 2	[3]
RP6530	DMYILGK	Chronic lymphocytic leukaemia	2A82.0	Phase 2	[3]
Parsaclisib	DMYBIFS	Follicular lymphoma	2A80	Phase 2	[9]
AZD8154	DMK13L1	Asthma	CA23	Phase 2	[10]

Drug(s) Targeting Casein kinase I epsilon (CSNK1E)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
IC261	DMXB95R	Pancreatic cancer	2C10	Preclinical	[11]
PF-4800567	DM8P9ST	Chronic lymphocytic leukaemia	2A82.0	Preclinical	[12]
PF-670462	DMTJBP9	Chronic lymphocytic leukaemia	2A82.0	Preclinical	[13]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Casein kinase I epsilon (CSNK1E)	TTA8PLI	KC1E_HUMAN	Inhibitor	[1]
PI3-kinase delta (PIK3CD)	TTGBPJE	PK3CD_HUMAN	Inhibitor	[1]

References

• [1] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021
• [2] ClinicalTrials.gov (NCT02793583) Study to Assess the Efficacy and Safety of Ublituximab + Umbralisib With or Without Bendamustine and Umbralisib Alone in Patients With Previously Treated Non-Hodgkins Lymphoma (UNITY-NHL). U.S. National Institutes of Health.
• [3] Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
• [4] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [5] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [6] PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
• [7] Effective "activated PI3K syndrome"-targeted therapy with the PI3K inhibitor leniolisib. Blood. 2017 Nov 23;130(21):2307-2316.
• [8] Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
• [9] Parsaclisib, a potent and highly selective PI3K inhibitor, in patients with relapsed or refractory B-cell malignancies. Blood. 2019 Apr 18;133(16):1742-1752.
• [10] Discovery of AZD8154, a Dual PI3Kgamma-delta Inhibitor for the Treatment of Asthma. J Med Chem. 2021 Jun 24;64(12):8053-8075.
• [11] Crystal structure of a conformation-selective casein kinase-1 inhibitor. J Biol Chem. 2000 Jun 30;275(26):20052-60.
• [12] Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9.
• [13] Casein kinase 1 is a therapeutic target in chronic lymphocytic leukemia. Blood. 2018 Mar 15;131(11):1206-1218.