DAROVASERTIB

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C22H23F3N8O
Molecular Weight	472.4662
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1(N)CCN(CC1)C2=CC=CN=C2NC(=O)C3=C(N)N=CC(=N3)C4=C(C=CC=N4)C(F)(F)F

InChI

InChIKey=XXJXHXJWQSCNPX-UHFFFAOYSA-N

InChI=1S/C22H23F3N8O/c1-21(27)6-10-33(11-7-21)15-5-3-9-29-19(15)32-20(34)17-18(26)30-12-14(31-17)16-13(22(23,24)25)4-2-8-28-16/h2-5,8-9,12H,6-7,10-11,27H2,1H3,(H2,26,30)(H,29,32,34)

HIDE SMILES / InChI

Molecular Formula	C22H23F3N8O
Molecular Weight	472.4662
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Protein kinase C, PKC; classical/novel 4 Target ID: CHEMBL2096620 Sources: https://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20160211&CC=WO&NR=2016020864A1&KC=A1	Inhibitor 8504

C_max

Value	Dose	Analyte	Population
776 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3540 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5580 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4970 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6080 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
5410 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
4070 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4350 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1190 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2500 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3860 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4170 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5110 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2910 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2860 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2100 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
8640 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
21600 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
51300 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
63400 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
66200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
78000 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
29200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
35200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
30400 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10400 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13200 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
30500 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
45700 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
48300 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	1000 mg 1 times / day multiple, oral dose: 1000 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16900 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
19100 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15900 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
8.49 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.52 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.2 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	500 mg single, oral dose: 500 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.85 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
10 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
13.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	300 mg 2 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/36624219/	400 mg 2 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	LXS-196 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:09:54 GMT 2025` Edited by `admin` on `Mon Mar 31 23:09:54 GMT 2025`
Record UNII	E0YF0M8O09
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

IDE-196

Preferred Name

English

DAROVASERTIB

Official Name

English

3-AMINO-N-(3-(4-AMINO-4-METHYLPIPERIDIN-1-YL)PYRIDIN-2-YL)-6-(3-(TRIFLUOROMETHYL)PYRIDIN-2-YL)PYRAZINE-2-CARBOXAMIDE

Systematic Name

English

2-PYRAZINECARBOXAMIDE, 3-AMINO-N-(3-(4-AMINO-4-METHYL-1-PIPERIDINYL)-2-PYRIDINYL)-6-(3-(TRIFLUOROMETHYL)-2-PYRIDINYL)-

Systematic Name

English

LXS196

Code

English

Darovasertib [WHO-DD]

Common Name

English

IDE196

Code

English

LXS-196

Code

English

DAROVASERTIB [USAN]

Common Name

English

NVP-LXS-196

Code

English

darovasertib [INN]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

873322