Golidocitinib

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C25H31N9O2
Molecular Weight	489.5727
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=NN(C)C=C1NC2=NC=CC(=N2)C3=CNC4=C3C=CC=C4NC(=O)[C@@H](C)N5CCN(C)CC5

InChI

InChIKey=CVCVOSPZEVINRM-MRXNPFEDSA-N

InChI=1S/C25H31N9O2/c1-16(34-12-10-32(2)11-13-34)23(35)28-20-7-5-6-17-18(14-27-22(17)20)19-8-9-26-25(29-19)30-21-15-33(3)31-24(21)36-4/h5-9,14-16,27H,10-13H2,1-4H3,(H,28,35)(H,26,29,30)/t16-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C25H31N9O2
Molecular Weight	489.5727
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Approval Year

C_max

Value	Dose	Analyte	Population
5.14 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.6 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
48.5 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
133 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
232 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
33.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
62.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
149 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
83.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
169 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
375 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
923 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2340 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5260 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7260 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
536 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1020 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2490 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1530 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	25 mg 1 times / day steady-state, oral dose: 25 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3190 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg 1 times / day steady-state, oral dose: 50 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7190 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
51.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
42.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
50.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
46.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
37% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/37077916/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		GOLIDOCITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Substance Class	Chemical Created by `admin` on `Wed Apr 02 02:21:04 GMT 2025` Edited by `admin` on `Wed Apr 02 02:21:04 GMT 2025`
Record UNII	3BY9Z3M34G
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AZD-4205

Preferred Name

English

Golidocitinib

Official Name

English

(?R)-N-[3-[2-[(3-Methoxy-1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-1H-indol-7-yl]-?,4-dimethyl-1-piperazineacetamide

Systematic Name

English

Golidocitinib [WHO-DD]

Common Name

English

GOLIDOCITINIB [USAN]

Common Name

English

1-Piperazineacetamide, N-[3-[2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-1H-indol-7-yl]-?,4-dimethyl-, (?R)-

Systematic Name

English

golidocitinib [INN]

Common Name

English

(R)-N-(3-{2-[(3-Methoxy-1-methyl-1H-pyrazol-4-yl)amino]pyrimidin-4-yl}-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide

Systematic Name

English

AZD4205

Code

English

Code System Code Type Description

INN

11820