BARICITINIB PHOSPHATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H17N7O2S.H3O4P
Molecular Weight	469.412
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OP(O)(O)=O.CCS(=O)(=O)N1CC(CC#N)(C1)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

InChI

InChIKey=FBPOWTFFUBBKBB-UHFFFAOYSA-N

InChI=1S/C16H17N7O2S.H3O4P/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14;1-5(2,3)4/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20);(H3,1,2,3,4)

HIDE SMILES / InChI

Description
Sources: http://www.ema.europa.eu/docs/en_GB/document_library/Summary_of_opinion_-_Initial_authorisation/human/004085/WC500218183.pdf | https://www.ncbi.nlm.nih.gov/pubmed/20363976 | https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000PharmR.pdf | https://www.drugs.com/history/baricitinib.html | https://www.ncbi.nlm.nih.gov/pubmed/27910962

Baricitinib (trade name Olumiant) is an investigational drug for rheumatoid arthritis (RA), being developed by Incyte and Eli Lilly. Baricitinib is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays. In February 2017 Baricitinib was approved for use in the European Union as a second-line therapy for moderate to severe active rheumatoid arthritis in adults, either alone or in combination with methotrexate. On 31 May 2018 FDA approved Barictinib for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response to one or more TNF antagonist therapies.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Tyrosine-protein kinase JAK3 27 Target ID: CHEMBL2148 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26372653	Inhibitor 8297	180.0 nM [IC50]
Tyrosine-protein kinase JAK1 38 Target ID: CHEMBL2835 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20363976	Inhibitor 8297	5.9 nM [IC50]
Tyrosine-protein kinase JAK2 55 Target ID: CHEMBL2971 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20363976	Inhibitor 8297	5.7 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Rheumatoid arthritis 316 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	Primary		Approved 8429	OLUMIANT Approved Use OLUMIANT is a Janus kinase (JAK) inhibitor indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response to one or more TNF antagonist therapies. Launch Date 2010

C_max

Value	Dose	Analyte	Population
36.2 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28749581	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	BARICITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
47.8 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03212638	4 mg single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status: Fasted
32.5 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03212638	4 mg single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status: High fat meal
136 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: oral experiment type: multiple co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
147 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	10 mg single, oral dose: 10 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
29 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02708095	2 mg 1 times / day steady, oral dose: 2 mg route of administration: oral experiment type: steady co-administered:	BARICITINIB plasma	Homo sapiens population: unhealthy age: sex: food status:
47.8 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	4 mg single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
48 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	4 mg 1 times / day multiple, oral dose: 4 mg route of administration: oral experiment type: multiple co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
59.2 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02708095	4 mg 1 times / day steady, oral dose: 4 mg route of administration: oral experiment type: steady co-administered:	BARICITINIB plasma	Homo sapiens population: unhealthy age: sex: food status:

AUC

Value	Dose	Analyte	Population
236 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28749581	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:	BARICITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
265 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	4 mg 1 times / day steady, oral dose: 4 mg route of administration: oral experiment type: steady co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
771 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	10 mg 1 times / day steady, oral dose: 10 mg route of administration: oral experiment type: steady co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
216 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03212638	4 mg single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status: Fasted
273 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT03212638	4 mg single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status: High fat meal
270 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	4 mg 1 times / day single, oral dose: 4 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:
777 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT02758613	10 mg 1 times / day single, oral dose: 10 mg route of administration: oral experiment type: single co-administered:	BARICITINIB plasma	Homo sapiens population: healthy age: sex: food status:

T_1/2

Value	Dose	Co-administered	Analyte	Population
7.28 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28749581	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:		BARICITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
50% EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/28749581	4 mg single, oral dose: 4 mg route of administration: Oral experiment type: SINGLE co-administered:		BARICITINIB plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

Doses

Dose	Population	Adverse events
20 mg 1 times / day multiple, oral Highest studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf https://pubmed.ncbi.nlm.nih.gov/24965573	healthy, 30.6 years (ramge: 18–55 years) n = 8 Health Status: healthy Age Group: 30.6 years (ramge: 18–55 years) Sex: M+F Population Size: 8 Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf https://pubmed.ncbi.nlm.nih.gov/24965573	Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf https://pubmed.ncbi.nlm.nih.gov/24965573
40 mg single, oral Highest studied dose Dose: 40 mg Route: oral Route: single Dose: 40 mg Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf Page: p. 10	healthy Health Status: healthy Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf Page: p. 10	Sources: https://ec.europa.eu/health/documents/community-register/2018/20180629141659/anx_141659_en.pdf Page: p. 10
2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	Other AEs: Pneumonia, Systemic herpes zoster infection... Other AEs: Pneumonia (serious\|grade 5) Systemic herpes zoster infection (serious\|grade 5) Urinary tract infection (serious\|grade 5) Venous thrombosis (serious\|grade 5) Pulmonary embolism (serious\|grade 5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 479 Health Status: unhealthy Population Size: 479 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	Disc. AE: Systemic herpes zoster infection, Anemia... AEs leading to discontinuation/dose reduction: Systemic herpes zoster infection (1%) Anemia (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171
4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 997 Health Status: unhealthy Population Size: 997 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	Disc. AE: Systemic herpes zoster infection, Infestation... AEs leading to discontinuation/dose reduction: Systemic herpes zoster infection (1%) Infestation (1.6%) Alanine aminotransferase increase (0.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171

AEs

AE	Significance	Dose	Population
Pneumonia	serious\|grade 5	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
Pulmonary embolism	serious\|grade 5	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
Systemic herpes zoster infection	serious\|grade 5	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
Urinary tract infection	serious\|grade 5	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
Venous thrombosis	serious\|grade 5	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/207924Orig1s000lbl.pdf
Anemia	0.6% Disc. AE	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 479 Health Status: unhealthy Population Size: 479 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171
Systemic herpes zoster infection	1% Disc. AE	2 mg 1 times / day steady, oral Recommended Dose: 2 mg, 1 times / day Route: oral Route: steady Dose: 2 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 479 Health Status: unhealthy Population Size: 479 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171
Alanine aminotransferase increase	0.2% Disc. AE	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 997 Health Status: unhealthy Population Size: 997 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171
Systemic herpes zoster infection	1% Disc. AE	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 997 Health Status: unhealthy Population Size: 997 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171
Infestation	1.6% Disc. AE	4 mg 1 times / day steady, oral Dose: 4 mg, 1 times / day Route: oral Route: steady Dose: 4 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171	unhealthy n = 997 Health Status: unhealthy Population Size: 997 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000MedR.pdf Page: p. 171

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587 inducer 781	substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OAT2 145 CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 P-gp 1461 OCT1 512 OCT2 647 OAT1 599 OAT3 642 OATP1B1 788 BCRP 699 OATP1B3 706 MATE2 263	CYP1A2 1054 CYP2B6 664 CYP2C8 693 CYP2C19 991 P-gp 1537 OAT1 326 OCT1 327 OCT2 355 OATP1B1 406 OAT3 339 BCRP 561 OATP1B3 350 MATE2 96	PXR 9

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
PXR 46	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	unlikely
OAT2 147	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 6.0	weak [IC50 100 uM]
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	weak [IC50 >25 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 11.6 uM]
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 60.0	yes [IC50 13.7 uM]	yes (co-administration study) Comment: transport of metformin was inhibited by LY3009104 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 60.0
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 49.4 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 50 uM]
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 6.9 uM]
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 8.4 uM]
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes [IC50 >100 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP1A2 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
OCT1 327	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	no
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes
MATE2 96	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 60.0	yes
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0	yes	yes (co-administration study) Comment: the bii-directional transport ratio of LY3009104 reduced in the presence of BCRP inhibitors Kol43, FTC, and GF120918 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 59.0
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 41, 59	yes	yes (co-administration study) Comment: uptake was inhibited by probenecid; probenecid increased baricitinib AUC by 2-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/207924Orig1s000ClinPharmR.pdf Page: 41, 59

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY459479	https://www.001chemical.com/chem/1187594-09-7
001 Chemical	DY509857	https://www.001chemical.com/chem/1187595-84-1
AA Blocks	AA003A32	https://www.aablocks.com/goods/Goods/detail?id=AA003A32
AEchem Scientific Corp., USA	AE049545	http://www.aechemsc.com/info_products/AE049545.php
AK Scientific, Inc. (AKSCI)	Y0439	http://www.aksci.com/item_detail.php?cat=Y0439
Aaron Chemicals	AR003AUU	http://www.aaronchem.com/1187594-09-7
AbMole Bioscience	M2039	http://www.abmole.com/products/baricitinib.html
Acadechem	ACDS-068229	http://www.acadechemical.com/product/142928
Achemtek	0102-013841	http://www.achemtek.com/1187594-09-7
Active Biopharma	ABP001023	http://www.activebiopharma.com/1187594-09-7
Adooq BioScience	A11329	https://www.adooq.com/baricitinib.html
Alsachim	4636	http://www.alsachim.com/product-C5984-glo.bal-view.html
Ambinter	Amb22370255	http://www.ambinter.com/reference/22370255
Ambinter	Amb22491663	http://www.ambinter.com/reference/22491663
Angel Pharmatech	AG-11289	http://www.angelpharmatech.com/1187594-09-7.html
Angene	AGN-PC-0WA3Y8	http://www.angenechemical.com/productshow/AGN-PC-0WA3Y8.html
ApexBio Technology	A4141	http://www.apexbt.com/baricitinib-ly3009104-incb028050.html
ApexBio Technology	A3222	http://www.apexbt.com/baricitinib-phosphate.html
Ark Pharm	AK143352	http://www.arkpharminc.com/products/1187594-09-7.html
Aurora Fine Chemicals LLC	A17.866.933	http://online.aurorafinechemicals.com/info?ID=A17.866.933
Aurum Pharmatech LLC	S-7686	http://www.Aurumpharmatech.com/Product/ProductDetails/S_7686
AvaChem Scientific	3630	http://www.avachem.com/productSearch.asp?3630
Axon MedChem	1955	https://www.axonmedchem.com/product/1955
Beijing Acemol Technology	AMMD00005	http://www.acemol.com/products/PAMMD00005.shtml
BioChemPartner	BCP04686	http://www.biochempartner.com/1187594-09-7-BCP04686
BioCrick	BCC2195	http://www.biocrick.com/Baricitinib-LY3009104-INCB028050-BCC2195.html
BioSynth	J-503551	https://www.biosynth.com/en/products/all-products/products/J-503551.html
Boerchem	BC600315	http://www.boerchem.com/?product_43150.html
Chem Scene	CS-0724	http://www.chemscene.com/1187594-09-7.html
ChemFish Tokyo co.,ltd	44205240	http://www.chemfish.co.jp/index.php?id=4622&project=product
Chemenu	CM105935	http://www.chemenu.com/products/CM105935
Chemspace	CSSB00015190072	https://chem-space.com/CSSB00015190072
Clearsynth	CS-T-48553	https://www.clearsynth.com/en/CST48553.html
DC Chemicals	DC5064	http://www.dcchemicals.com/product_show-Baricitinib_INCB28050_LY3009104_.html
Excenen	EX-A413	http://www.excenen.com/searchresultlist.php?id=1187594-09-7
Finetech	FT-0775037	https://www.finetechnology-ind.com/prod/detail/pub/1187594-09-7.html
Matrix Scientific	112533	https://www.matrixscientific.com/112533.html
MedChem Express	HY-15315	https://www.medchemexpress.com/Baricitinib.html
Molcore	MC459479	https://www.molcore.com/product/1187594-09-7
Molcore	MC509857	https://www.molcore.com/product/1187595-84-1
Renno Tech	RL00725	http://www.rennotech.com/product_show.asp?id=264
Shanghai Send Pharmaceutical Technology Co., Ltd	send21141	http://shsendpharm.com/
Sinfoo Biotech	S052572	http://www.sinfoobiotech.com/product/1055970
Smolecule	S001993	http://www.smolecule.com/products/s001993
Smolecule	S520451	http://www.smolecule.com/products/s520451
Sun-shine Chemical	Baricitinib	http://www.sun-shinechem.com/1187594-09-7.html
Synblock Inc	SB10845	http://www.synblock.com/product/1187594-09-7.html
Synblock Inc	PB27275	http://www.synblock.com/product/1187595-84-1.html
THE BioTek	bt-253529	https://www.thebiotek.com/product/inhibitors/bt-253529
THE BioTek	bt-260938	https://www.thebiotek.com/product/inhibitors/bt-260938
Yuhao Chemical	RT14510	http://www.chemyuhao.com/1187594-09-7.html
abcr GmbH	AB453191	http://www.abcr.com/shop/en/AB453191
eNovation Chemicals	D372447	http://www.enovationchem.com/productDetails.asp?productID=D372447
eNovation Chemicals	D621217	https://www.enovationchem.com/ProductDetails.asp?ProductID=D621217
iChemical	EBD2199373	http://www.ichemical.com/products/1187594-09-7.html

PubMed

Title	Date	PubMed
		252160600
Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050.	2010 May 1	20363976

Patents

Sample Use Guides

In Vivo Use Guide

Baricitinib 2 mg administered orally once daily.

Route of Administration: Oral

In Vitro Use Guide

Baricitinib inhibits IL-6–stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively, in PBMCs. Baricitinib also inhibits pSTAT3 stimulated by IL-23 with IC50 of 20 nM in isolated naive T-cells

Name

Type

Language

BARICITINIB PHOSPHATE

Common Name

English

3-AZETIDINEACETONITRILE, 1-(ETHYLSULFONYL)-3-(4-(7H-PYRROLO(2,3-D)PYRIMIDIN-4-YL)-1H-PYRAZOL-1-YL)-, PHOSPHATE (1:1)

Systematic Name

English

BARICITINIB PHOSPHATE SALT

Common Name

English

INCB-28050

Code

English

Code System Code Type Description

CAS

1187595-84-1