Umbralisib

Umbralisib
Clinical data
Trade names	Ukoniq
Other names	RP5264; TGR-1202
AHFS/Drugs.com	Ukoniq
License data	US DailyMed: Umbralisib;
Pregnancy; category	Not recommended;
Routes of; administration	By mouth
ATC code	L01EX25 (WHO) ;
Legal status
Legal status	US: ℞-only / withdrawn;
Pharmacokinetic data
Metabolism	CYP2C9, CYP3A4, and CYP1A2
Elimination half-life	91 h
Excretion	Feces, urine
Identifiers
	IUPAC name 2-[(1S)-1-[4-Amino-3-(3-fluoro-4-propan-2-yloxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)chromen-4-one;
CAS Number	1532533-67-7;
PubChem CID	72950888;
DrugBank	DB14989;
ChemSpider	34979945;
UNII	38073MQB2A;
KEGG	D11322;
ChEMBL	ChEMBL3948730;
CompTox Dashboard (EPA)	DTXSID601337137 ;
Chemical and physical data
Formula	C31H24F3N5O3
Molar mass	571.560 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC(C)OC1=C(C=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F;
	InChI InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1; Key:IUVCFHHAEHNCFT-INIZCTEOSA-N;

Umbralisib, sold under the brand name Ukoniq, is an anti-cancer medication for the treatment of marginal zone lymphoma (MZL) and follicular lymphoma (FL). It is taken by mouth.

Umbralisib is a kinase inhibitor including PI3K-delta and casein kinase CK1-epsilon.

The most common side effects include increased creatinine, diarrhea-colitis, fatigue, nausea, neutropenia, transaminase elevation, musculoskeletal pain, anemia, thrombocytopenia, upper respiratory tract infection, vomiting, abdominal pain, decreased appetite, and rash.

Umbralisib was granted accelerated approval for medical use in the United States in February 2021. However, due to concerns for increased long term side effects leading to inferior overall survival which led to increased FDA scrutiny in the form of an ODAC review, it has been withdrawn from the US market.