NERATINIB

Details

Stereochemistry	ACHIRAL
Molecular Formula	C30H29ClN6O3
Molecular Weight	557.043
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC1=C(NC(=O)\C=C\CN(C)C)C=C2C(=C1)N=CC(C#N)=C2NC3=CC=C(OCC4=NC=CC=C4)C(Cl)=C3

InChI

InChIKey=JWNPDZNEKVCWMY-VQHVLOKHSA-N

InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+

HIDE SMILES / InChI

Molecular Formula	C30H29ClN6O3
Molecular Weight	557.043
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: http://adisinsight.springer.com/drugs/800021154
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26089701 | https://www.ncbi.nlm.nih.gov/pubmed/15715478

Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Receptor protein-tyrosine kinase erbB-2 35 Target ID: CHEMBL1824 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15715478	Inhibitor 8146		59.0 nM [IC50]
Epidermal growth factor receptor erbB1 57 Target ID: CHEMBL203 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15715478	Inhibitor 8146		92.0 nM [IC50]

Conditions

Condition	Modality	Highest Phase	Product
HER2-overexpressed/amplified breast cancer 3 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf	Primary	Approved 8307	NERLYNX Approved Use NERLYNX is indicated for the extended adjuvant treatment of adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab based therapy. Launch Date 1.50016321E12
Breast cancer 426 Sources: http://adisinsight.springer.com/drugs/800021154	Primary	Phase III 651	Unknown Approved Use Unknown
Non-small cell lung cancer 197 Sources: http://adisinsight.springer.com/drugs/800021154	Primary	Phase II 1133	Unknown Approved Use Unknown
Colorectal cancer 97 Sources: http://adisinsight.springer.com/drugs/800021154	Primary	Phase II 1133	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
73.1 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
81.5 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
76.3 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
71.8 ng/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

AUC

Value	Dose	Analyte	Population
1060 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
1110 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
1640 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
891 ng × h/mL REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

T_1/2

Value	Dose	Analyte	Population
14.6 h REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
22.7 h REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg 1 times / day steady-state, oral dose: 240 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
14.3 h REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FED
12.6 h REVIEW https://www.ncbi.nlm.nih.gov/pubmed/27284682	240 mg single, oral dose: 240 mg route of administration: Oral experiment type: SINGLE co-administered:	NERATINIB blood	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf			NERATINIB plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
400 mg 1 times / day steady, oral Highest studied dose Dose: 400 mg, 1 times / day Route: oral Route: steady Dose: 400 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	unhealthy, 49.5 years (range: 42-63 years) n = 6 Health Status: unhealthy Condition: Non–small cell lung cancer \| breast cancer Age Group: 49.5 years (range: 42-63 years) Sex: M+F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	DLT: Diarrhea... Disc. AE: Fatigue... Dose limiting toxicities: Diarrhea (grade 3, 3 patients) AEs leading to discontinuation/dose reduction: Fatigue (all grades, 5 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/19318484
240 mg 1 times / day steady, oral Recommended Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf	unhealthy, 52 years n = 1408 Health Status: unhealthy Condition: HER2-positive early-stage breast cancer Age Group: 52 years Sex: F Population Size: 1408 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf	DLT: Diarrhea, Diarrhea... Dose limiting toxicities: Diarrhea (all grades, 95%) Diarrhea (grade 3, 40%) Diarrhea (grade 4, 0.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf
240 mg 1 times / day steady, oral Recommended Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf	unhealthy, 52 years n = 1408 Health Status: unhealthy Condition: HER2-positive early-stage breast cancer Age Group: 52 years Sex: F Population Size: 1408 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf	Disc. AE: Nausea, Abdominal pain... Other AEs: Nausea, Abdominal pain... AEs leading to discontinuation/dose reduction: Nausea (grade 3, 2%) Abdominal pain (grade 3, 2%) Abdominal pain upper (grade 3, 2%) Abdominal pain lower (grade 3, 2%) Vomiting (grade 3, 3%) Fatigue (grade 3, 2%) Alanine aminotransferase increased (grade 3, 1%) Alanine aminotransferase increased (grade 4, 0.2%) Other AEs: Nausea (all grades, 43%) Abdominal pain (all grades, 36%) Abdominal pain upper (all grades, 36%) Abdominal pain lower (all grades, 36%) Vomiting (all grades, 26%) Stomatitis (all grades, 14%) Aphthous stomatitis (all grades, 14%) Mouth ulceration (all grades, 14%) Oral mucosal blistering (all grades, 14%) Mucosal inflammation (all grades, 14%) Oropharyngeal pain (all grades, 14%) Oral pain (all grades, 14%) Glossodynia (all grades, 14%) Glossitis (all grades, 14%) Cheilitis (all grades, 14%) Stomatitis (grade 3, 0.3%) Aphthous stomatitis (grade 3, 0.3%) Mouth ulceration (grade 3, 0.3%) Oral mucosal blistering (grade 3, 0.3%) Mucosal inflammation (grade 3, 0.3%) Oropharyngeal pain (grade 3, 0.3%) Oral pain (grade 3, 0.3%) Glossodynia (grade 3, 0.3%) Glossitis (grade 3, 0.3%) Cheilitis (grade 3, 0.3%) Dyspepsia (all grades, 10%) Dyspepsia (grade 3, 0.4%) Abdominal distension (all grades, 5%) Abdominal distension (grade 3, 0.3%) Dry mouth (all grades, 3%) Dry mouth (grade 3, 0.1%) Fatigue (all grades, 27%) Alanine aminotransferase increased (all grades, 9%) Aspartate aminotransferase increased (all grades, 7%) Aspartate aminotransferase increased (grade 3, 0.5%) Aspartate aminotransferase increased (grade 4, 0.2%) Urinary tract infection (all grades, 5%) Urinary tract infection (grade 3, 0.1%) Weight decreased (all grades, 5%) Weight decreased (grade 3, 0.1%) Decreased appetite (all grades, 12%) Decreased appetite (grade 3, 0.2%) Dehydration (all grades, 4%) Dehydration (grade 3, 0.9%) Dehydration (grade 4, 0.1%) Muscle spasms (all grades, 11%) Muscle spasms (grade 3, 0.1%) Epistaxis (all grades, 5%) Rash (all grades, 18%) Rash erythematous (all grades, 18%) Rash follicular (all grades, 18%) Generalized rash (all grades, 18%) Rash pruritic (all grades, 18%) Rash pustular (all grades, 18%) Maculopapular rash (all grades, 18%) Rash papular (all grades, 18%) Dermatitis (all grades, 18%) Dermatitis acneiform (all grades, 18%) Toxic skin eruption (all grades, 18%) Rash (grade 3, 0.6%) Rash erythematous (grade 3, 0.6%) Rash follicular (grade 3, 0.6%) Generalized rash (grade 3, 0.6%) Rash pruritic (grade 3, 0.6%) Rash pustular (grade 3, 0.6%) Maculopapular rash (grade 3, 0.6%) Rash papular (grade 3, 0.6%) Dermatitis (grade 3, 0.6%) Dermatitis acneiform (grade 3, 0.6%) Toxic skin eruption (grade 3, 0.6%) Dry skin (all grades, 6%) Nail disorder (all grades, 8%) Paronychia (all grades, 8%) Onychoclasis (all grades, 8%) Nail discoloration (all grades, 8%) Nail toxicity (all grades, 8%) Nail growth abnormal (all grades, 8%) Nail dystrophy (all grades, 8%) Nail disorder (grade 3, 0.3%) Paronychia (grade 3, 0.3%) Onychoclasis (grade 3, 0.3%) Nail discoloration (grade 3, 0.3%) Nail toxicity (grade 3, 0.3%) Nail growth abnormal (grade 3, 0.3%) Nail dystrophy (grade 3, 0.3%) Skin fissures (all grades, 2%) Skin fissures (grade 3, 0.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208051s000lbl.pdf
240 mg 1 times / day steady, oral Recommended Dose: 240 mg, 1 times / day Route: oral Route: steady Dose: 240 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf Page: p. 117	unhealthy, 52 years n = 1408 Health Status: unhealthy Condition: HER2-positive early-stage breast cancer Age Group: 52 years Sex: F Population Size: 1408 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf Page: p. 117	Other AEs: Bilirubin increased, Bilirubin increased... Other AEs: Bilirubin increased (all grades, 11.1%) Bilirubin increased (grade 3, 0.1%) Alkaline phosphatase (all grades, 22.7%) Creatinine increased (all grades, 12.5%) Creatinine increased (grade 4, 0.1%) Creatinine increased (grade 3, 0.1%) Hypercalcemia (all grades, 11.2%) Hypercalcemia (grade 4, 0.2%) Hypercalcemia (grade 3, 0.4%) Hypermagnesemia (all grades, 5.2%) Hypermagnesemia (grade 4, 0.1%) Hypermagnesemia (grade 3, 0.9%) Hypernatremia (all grades, 10.3%) Hypernatremia (grade 4, 0.1%) Hypernatremia (grade 3, 0.1%) Hypoalbuminemia (all grades, 8.4%) Hypoalbuminemia (grade 3, 0.1%) Hypocalcemia (all grades, 48.9%) Hypocalcemia (grade 4, 0.9%) Hypocalcemia (grade 3, 0.1%) Hypokalemia (all grades, 7.5%) Hypokalemia (grade 4, 0.1%) Hypokalemia (grade 3, 0.3%) Hypomagnesemia (all grades, 7.2%) Hypomagnesemia (grade 4, 0.2%) Hypomagnesemia (grade 3, 0.4%) Hyponatremia (all grades, 11.6%) Hyponatremia (grade 3, 0.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf Page: p. 117
180 mg 1 times / day steady, oral Dose: 180 mg, 1 times / day Route: oral Route: steady Dose: 180 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	unhealthy, 56.5 years (range: 46-90 years) n = 6 Health Status: unhealthy Condition: Breast cancer Age Group: 56.5 years (range: 46-90 years) Sex: F Population Size: 6 Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	DLT: Diarrhea... Disc. AE: Fatigue... Dose limiting toxicities: Diarrhea (grade 3, 1 patient) AEs leading to discontinuation/dose reduction: Fatigue (all grades, 1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/19318484
320 mg 1 times / day steady, oral MTD Dose: 320 mg, 1 times / day Route: oral Route: steady Dose: 320 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	unhealthy, 57 years (range: 34-80 years) n = 39 Health Status: unhealthy Condition: cancers Age Group: 57 years (range: 34-80 years) Sex: M+F Population Size: 39 Sources: https://pubmed.ncbi.nlm.nih.gov/19318484	Disc. AE: Diarrhea, Fatigue... Other AEs: Abdominal pain, Nausea... AEs leading to discontinuation/dose reduction: Diarrhea (all grades, 92%) Fatigue (all grades, 49%) Other AEs: Abdominal pain (all grades, 21%) Nausea (all grades, 54%) Vomiting (all grades, 49%) Anorexia (all grades, 33%) Rash (all grades, 8%) Sources: https://pubmed.ncbi.nlm.nih.gov/19318484

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1670 inhibitor 1532 inducer 753	inhibitor 1695 inducer 372	inhibitor 1789	inhibitor 1570

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
P-gp 1401 CYP2C19 1410 CYP1A2 1463 CYP2B6 770 L-type Ca channels 9	FMO 35 CYP3A 188	CYP1A2 671 CYP2B6 521

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1620	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP1A2 1620	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2B6 946	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2B6 946	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2C19 1484	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2C9 1747	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2C9 1747	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP2D6 1826	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP3A4 1857	inducer 1515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
CYP3A4 1857	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=68 Page: -	no
P-gp 1588	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=67 Page: -	yes [IC50 1 uM]	yes (co-administration study) Comment: NERATINIB increases digoxin Cmax& AUC Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=67 Page: -
L-type Ca channels 9	inhibitor 3185 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=34 Page: -	yes [Inhibition 10 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1670	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=65 Page: -	major	yes (co-administration study) Comment: ketoconazole increased Cmax and AUC by 3.2- and 4.8-fold respectively, rifampin (a strong CYP3A4 inducer) decreased the Cmax and AUC of neratinib by 76% and 87%, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=65 Page: -
FMO 35	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=65 Page: -	minor
CYP3A 188	substrate 3264 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=65 Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1603	inhibitor 1584 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208051Orig1s000MultidisciplineR.pdf#page=37 Page: -

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:61397	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:61397
ChemicalBook	CB2855051	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2855051
MolPort	MolPort-006-069-389	https://www.molport.com/shop/molecule-link/MolPort-006-069-389
Selleck Chemicals	Neratinib(HKI-272)	http://www.selleckchem.com/products/Neratinib(HKI-272).html
ZINC	ZINC000003916214	http://zinc15.docking.org/substances/ZINC000003916214
eMolecules	24195283	https://www.emolecules.com/cgi-bin/more?vid=24195283

PubMed

Title	Date	PubMed
		252160222
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.	2010 Nov 24	21095574
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.	2011 Mar 10	21322567
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.	2013 Nov	23956101

Patents

Sample Use Guides

In Vivo Use Guide

Patients who received 40, 80, or 120 mg experienced no dose-limiting toxicities. The study determined the maximum tolerated dose at 320 mg, with 240 mg being the therapeutic dose.

Route of Administration: Oral

In Vitro Use Guide

both very low (10 nM) and physiologically attainable concentrations of neratinib (133 nM) significantly inhibited the autophosphorylation of HER2/neu and activation of S6 in primary carcinosarcoma cells

Substance Class	Chemical Created by `admin` on `Fri Dec 16 20:07:21 UTC 2022` Edited by `admin` on `Fri Dec 16 20:07:21 UTC 2022`
Record UNII	JJH94R3PWB
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

NERATINIB

Official Name

English

2-BUTENAMIDE, N-(4-((3-CHLORO-4-(2-PYRIDINYLMETHOXY)PHENYL)AMINO)-3-CYANO-7-ETHOXY-6-QUINOLINYL)-4-(DIMETHYLAMINO)-, (2E)-

Systematic Name

English

HKI-272

Code

English

CDP-820

Code

English

NERATINIB [MART.]

Common Name

English

NERATINIB [MI]

Common Name

English

NERATINIB [USAN]

Common Name

English

neratinib [INN]

Common Name

English

Neratinib [WHO-DD]

Common Name

English

(2E)-N-[4-[[3-Chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

699119