TUCATINIB HEMIETHANOLATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	2C26H24N8O2.C2H6O
Molecular Weight	1007.1108
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCO.CC1=C(OC2=CC3=NC=NN3C=C2)C=CC(NC4=NC=NC5=C4C=C(NC6=NC(C)(C)CO6)C=C5)=C1.CC7=C(OC8=CC9=NC=NN9C=C8)C=CC(NC%10=NC=NC%11=C%10C=C(NC%12=NC(C)(C)CO%12)C=C%11)=C7

InChI

InChIKey=UGAFQGGOUGJBMF-UHFFFAOYSA-N

InChI=1S/2C26H24N8O2.C2H6O/c2*1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25;1-2-3/h2*4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31);3H,2H2,1H3

HIDE SMILES / InChI

Description
Sources: http://www.arraybiopharma.com/product-pipeline/other-compounds/arry-380-ont-380/ | https://www.ncbi.nlm.nih.gov/pubmed/27249772

TUCATINIB (ONT-380 or ARRY-380) is an orally active, reversible and selective small-molecule HER2 inhibitor invented by Array and licensed to Cascadian Therapeutics (previously named Oncothyreon) for development, manufacturing and commercialization. HER2, a growth factor receptor that is over-expressed in multiple cancers, including breast, ovarian, and stomach cancer. HER2 mediates cell growth, differentiation and survival, and tumors that overexpress HER2 are more aggressive and historically have been associated with poorer overall survival compared with HER2-negative cancers. ONT-380 is highly active as a single agent and in combination with both chemotherapy and Herceptin® (trastuzumab) in xenograft models of HER2+ breast cancer, including models of CNS metastases that were refractory to Tykerb® (lapatinib) or neratinib treatment. In a Phase 1 single agent clinical study, ONT-380 administered orally twice a day was well tolerated and demonstrated anti-tumor activity in heavily pre-treated HER2+ breast cancer patients with metastatic disease. Based on the strength of these preclinical and clinical trials, ONT-380 is advancing in one Phase 2 and three Phase 1b combination trials in patients with metastatic breast cancer. A second study reported the CNS activity of ONT-380 in combination with either T-DM1 or trastuzumab or capecitabine. Patients with brain metastases assessable for response were included in the combined analysis. Responses and clinical benefit in the CNS were reported with the three combinations tested, supporting future development of the drug for this particular indication.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Receptor protein-tyrosine kinase erbB-2 35 Target ID: CHEMBL1824 Sources: https://adisinsight.springer.com/drugs/800021257 \| http://www.arraybiopharma.com/product-pipeline/other-compounds/arry-380-ont-380/	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Breast cancer 434 Sources: http://adisinsight.springer.com/drugs/800021257 https://www.ncbi.nlm.nih.gov/pubmed/28053022 https://www.ncbi.nlm.nih.gov/pubmed/27249772	Primary		Phase II 1132	Unknown Approved Use Unknown
Colorectal cancer 101 Sources: https://clinicaltrials.gov/ct2/show/NCT03043313	Primary		Phase II 1132	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
790 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29955792	300 mg 2 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TUCATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
2920 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29955792	300 mg 2 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TUCATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
5.5 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/29955792	300 mg 2 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TUCATINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
2.9% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf			TUCATINIB plasma	Homo sapiens

Doses

Dose	Population	Adverse events
300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Co-administed with:: trastuzumab(loading dose of 8 mg/kg on Day 1 of Cycle 1 if needed and then a maintenance dose of 6 mg/kg on Day 1 of every 21-day cycle) capecitabine(1000 mg/m2 orally twice daily on Days 1 through 14 of every 21-day cycle) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	unhealthy, 54 years (range: 22 - 82 years) n = 404 Health Status: unhealthy Age Group: 54 years (range: 22 - 82 years) Sex: M+F Population Size: 404 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	Disc. AE: Hepatotoxicity, Diarrhea... AEs leading to discontinuation/dose reduction: Hepatotoxicity (1.5%) Diarrhea (1%) Hepatotoxicity (8%) Diarrhea (6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf
800 mg 2 times / day steady, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: steady Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053023	unhealthy, 58 years (range: 31–77 years) n = 4 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/28053023	DLT: Alanine aminotransferase increased, Aspartate aminotransferase increased... Dose limiting toxicities: Alanine aminotransferase increased (grade 3, 2 patients) Aspartate aminotransferase increased (grade 3, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/28053023
600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	Other AEs: Diarrhea, Nausea... Other AEs: Diarrhea (grade 1-2, 26%) Nausea (grade 1-2, 33%) Fatigue (grade 1-2, 19%) Vomiting (grade 1-2, 3%) Acne (grade 3, 4%) Dermatitis acneiform (grade 3, 4%) Skin exfoliation (grade 3, 4%) Alanine aminotransferase increased (grade 3, 4%) Aspartate aminotransferase increased (grade 2, 11%) Sources: https://pubmed.ncbi.nlm.nih.gov/28053022

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inhibitor 1767		inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 214 CYP2C8 911 OCT2 647 MATE1 306 MATE2 263 P-gp 1461	CYP2C8 693 CYP3A 191 P-gp 1537 BCRP 561

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83	yes [IC50 20 uM]	yes (co-administration study) Comment: Digoxin Cmax increased by 2.4-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83	yes [Ki 0.135 uM]	yes (co-administration study) Comment: Metformin Cmax increased by 1.1-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83	yes [Ki 0.17 uM]	yes (co-administration study) Comment: Repaglinide Cmax increased by 1.7-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83	yes [Ki 0.34 uM]	yes (co-administration study) Comment: Metformin Cmax increased by 1.1-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81, 83
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83	yes [Ki 0.805 uM]	yes (co-administration study) Comment: Midazolam Cmax increased by 3-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81.0	yes [Ki 14.7 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83	yes [Ki 4.57 uM]	no (co-administration study) Comment: No effect on tolbutamide Cmax or AUC Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83

Drug as victim

Target	Modality	Activity	Clinical evidence
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81.0	yes
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 81.0	yes
CYP3A 191	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83	yes	weak (co-administration study) Comment: Itraconazole increased tucatinib Cmax by 1.3-fold; Rifampin decreased tucatinib Cmax by 37% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83	yes	yes (co-administration study) Comment: Gemfibrozil increased tucatinib Cmax by 1.6-fold; Rifampin decreased tucatinib Cmax by 37% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 80, 83

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213411Orig1s000MultidisciplineR.pdf Page: 39.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY581239	https://www.001chemical.com/chem/937263-43-9
AA Blocks	AA00GTX3	https://www.aablocks.com/goods/Goods/detail?id=AA00GTX3
Aaron Chemicals	AR00GUOV	http://www.aaronchem.com/937263-43-9
AbMole Bioscience	M10038	http://www.abmole.com/products/tucatinib.html
Achemtek	0102-014230	http://www.achemtek.com/937263-43-9
Adooq BioScience	A16413	https://www.adooq.com/arry-380-23502.html
Ambinter	Amb24123281	http://www.ambinter.com/reference/24123281
Angel Pharmatech	AG-19862	http://www.angelpharmatech.com/937263-43-9.html
Ark Pharm	AK548135	http://www.arkpharminc.com/products/937263-43-9.html
Ark Pharma Scientific Limited	A-0731	http://www.arkpharmtech.com/product/32682.html
BioChemPartner	BCP15983	http://www.biochempartner.com/937263-43-9-BCP15983
Boerchem	BC600725	http://www.boerchem.com/?product_43560.html
Chem Scene	CS-3906	http://www.chemscene.com/937263-43-9.html
Chemspace	CSSB00020668746	https://chem-space.com/CSSB00020668746
DC Chemicals	DC8771	http://www.dcchemicals.com/product_show-Irbinitinib_ARRY_380_.html
Debye Scientific	DB-130430	http://www.debyesci.com/cas_937263-43-9.html
Excenen	EX-A1031	http://www.excenen.com/searchresultlist.php?id=937263-43-9
Lab Network	LN01288250	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01288250
MedChem Express	HY-16069	https://www.medchemexpress.com/Irbinitinib.html
Molcore	MC581239	https://www.molcore.com/product/937263-43-9
Smolecule	S547973	http://www.smolecule.com/products/s547973
Sun-shine Chemical	Irbinitinib	http://www.sun-shinechem.com/Details/Irbinitinib/2223/937263-43-9.html
Synblock Inc	SB17126	http://www.synblock.com/product/937263-43-9.html
THE BioTek	bt-287490	https://www.thebiotek.com/product/inhibitors/bt-287490
Yuhao Chemical	RT10803	http://www.chemyuhao.com/937263-43-9.html
abcr GmbH	AB479024	http://www.abcr.com/shop/en/AB479024
eNovation Chemicals	D501838	https://www.enovationchem.com/ProductDetails.asp?ProductID=D501838
eNovation Chemicals	D549339	https://www.enovationchem.com/ProductDetails.asp?ProductID=D549339
eNovation Chemicals	Y0974435	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0974435

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

Phase 2 Study of tucatinib in combination with capecitabine & trastuzumab in patients with advanced HER2+ breast cancer: Tucatinib 300 mg or placebo will be given orally twice daily (PO BID).

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

TUCATINIB HEMIETHANOLATE

Common Name

English

ETHANOL, COMPD. WITH N6-(4,5-DIHYDRO-4,4-DIMETHYL-2-OXAZOLYL)-N4-(3-METHYL-4-((1,2,4)TRIAZOLO(1,5-A)PYRIDIN-7-YLOXY)PHENYL)-4,6-QUINAZOLINEDIAMINE (1:2)

Systematic Name

English

Code System Code Type Description

FDA UNII

CDZ29KT2FT

Created by admin on Sat Dec 16 18:07:32 GMT 2023 , Edited by admin on Sat Dec 16 18:07:32 GMT 2023

PRIMARY

CAS

1429755-56-5

Created by admin on Sat Dec 16 18:07:32 GMT 2023 , Edited by admin on Sat Dec 16 18:07:32 GMT 2023

PRIMARY

SMS_ID

300000024838

Created by admin on Sat Dec 16 18:07:32 GMT 2023 , Edited by admin on Sat Dec 16 18:07:32 GMT 2023

PRIMARY

PUBCHEM

162623678

Created by admin on Sat Dec 16 18:07:32 GMT 2023 , Edited by admin on Sat Dec 16 18:07:32 GMT 2023

PRIMARY

ACTIVE MOIETY


					234248D0HH

TUCATINIB

SUBSTANCE RECORD


					CDZ29KT2FT

TUCATINIB HEMIETHANOLATE

AE	Significance	Dose	Population
Diarrhea	1% Disc. AE	300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Co-administed with:: trastuzumab(loading dose of 8 mg/kg on Day 1 of Cycle 1 if needed and then a maintenance dose of 6 mg/kg on Day 1 of every 21-day cycle) capecitabine(1000 mg/m2 orally twice daily on Days 1 through 14 of every 21-day cycle) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	unhealthy, 54 years (range: 22 - 82 years) n = 404 Health Status: unhealthy Age Group: 54 years (range: 22 - 82 years) Sex: M+F Population Size: 404 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf
Hepatotoxicity	1.5% Disc. AE	300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Co-administed with:: trastuzumab(loading dose of 8 mg/kg on Day 1 of Cycle 1 if needed and then a maintenance dose of 6 mg/kg on Day 1 of every 21-day cycle) capecitabine(1000 mg/m2 orally twice daily on Days 1 through 14 of every 21-day cycle) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	unhealthy, 54 years (range: 22 - 82 years) n = 404 Health Status: unhealthy Age Group: 54 years (range: 22 - 82 years) Sex: M+F Population Size: 404 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf
Diarrhea	6% Disc. AE	300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Co-administed with:: trastuzumab(loading dose of 8 mg/kg on Day 1 of Cycle 1 if needed and then a maintenance dose of 6 mg/kg on Day 1 of every 21-day cycle) capecitabine(1000 mg/m2 orally twice daily on Days 1 through 14 of every 21-day cycle) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	unhealthy, 54 years (range: 22 - 82 years) n = 404 Health Status: unhealthy Age Group: 54 years (range: 22 - 82 years) Sex: M+F Population Size: 404 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf
Hepatotoxicity	8% Disc. AE	300 mg 2 times / day steady, oral Recommended Dose: 300 mg, 2 times / day Route: oral Route: steady Dose: 300 mg, 2 times / day Co-administed with:: trastuzumab(loading dose of 8 mg/kg on Day 1 of Cycle 1 if needed and then a maintenance dose of 6 mg/kg on Day 1 of every 21-day cycle) capecitabine(1000 mg/m2 orally twice daily on Days 1 through 14 of every 21-day cycle) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf	unhealthy, 54 years (range: 22 - 82 years) n = 404 Health Status: unhealthy Age Group: 54 years (range: 22 - 82 years) Sex: M+F Population Size: 404 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213411s000lbl.pdf
Alanine aminotransferase increased	grade 3, 2 patients DLT, Disc. AE	800 mg 2 times / day steady, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: steady Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053023	unhealthy, 58 years (range: 31–77 years) n = 4 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/28053023
Aspartate aminotransferase increased	grade 3, 2 patients DLT, Disc. AE	800 mg 2 times / day steady, oral Highest studied dose Dose: 800 mg, 2 times / day Route: oral Route: steady Dose: 800 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053023	unhealthy, 58 years (range: 31–77 years) n = 4 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 4 Sources: https://pubmed.ncbi.nlm.nih.gov/28053023
Fatigue	grade 1-2, 19%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Diarrhea	grade 1-2, 26%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Vomiting	grade 1-2, 3%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Nausea	grade 1-2, 33%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Aspartate aminotransferase increased	grade 2, 11%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Acne	grade 3, 4%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Alanine aminotransferase increased	grade 3, 4%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Dermatitis acneiform	grade 3, 4%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022
Skin exfoliation	grade 3, 4%	600 mg 2 times / day steady, oral MTD Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28053022	unhealthy, 58 years (range: 31–77 years) n = 27 Health Status: unhealthy Age Group: 58 years (range: 31–77 years) Sex: M+F Population Size: 27 Sources: https://pubmed.ncbi.nlm.nih.gov/28053022

Details

SMILES

InChI

DescriptionSources: http://www.arraybiopharma.com/product-pipeline/other-compounds/arry-380-ont-380/ | https://www.ncbi.nlm.nih.gov/pubmed/27249772

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Approved Use

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.arraybiopharma.com/product-pipeline/other-compounds/arry-380-ont-380/ | https://www.ncbi.nlm.nih.gov/pubmed/27249772

C_max

T_1/2

F_unbound

Drug as perpetrator