MAVELERTINIB

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C18H22FN9O2
Molecular Weight	415.4248
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=NN(C)C=C1NC2=C3N=CN(C)C3=NC(=N2)N4C[C@@H](F)[C@@H](C4)NC(=O)C=C

InChI

InChIKey=JYIUNVOCEFIUIU-GHMZBOCLSA-N

InChI=1S/C18H22FN9O2/c1-5-13(29)21-11-8-28(6-10(11)19)18-23-15(14-16(24-18)26(2)9-20-14)22-12-7-27(3)25-17(12)30-4/h5,7,9-11H,1,6,8H2,2-4H3,(H,21,29)(H,22,23,24)/t10-,11-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C18H22FN9O2
Molecular Weight	415.4248
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	2 / 2
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28287730

PF-06747775 is an irreversible pyrrolopyrimidine inhibitor of epidermal growth factor receptor (EGFR) T790M mutants which provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties. The third-generation class of EGFR tyrosine kinase inhibitors PF-06747775 is a clinical candidate drug for treatment of non-small-cell lung cancer (NSCLC) driven by mutant EGFR.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Epidermal growth factor receptor 49 Target ID: P00533\|\|\|Q9GZX1 Gene ID: 1956.0 Gene Symbol: EGFR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/28287730	Inhibitor 8504		3.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Non-small cell lung cancer 211 Sources: https://clinicaltrials.gov/ct2/show/NCT02349633	Primary		Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
2242 ng/mL CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/35657653/	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:		MAVELERTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2829 ng/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT02349633	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:		MAVELERTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
9536 ng × h/mL CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/35657653/	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:		MAVELERTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
19990 ng × h/mL CLINICAL TRIAL https://clinicaltrials.gov/study/NCT02349633	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:		MAVELERTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
6.87 h CLINICAL TRIAL https://pubmed.ncbi.nlm.nih.gov/35657653/	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:		MAVELERTINIB plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6 h EXPERIMENT https://www.jto.org/article/S1556-0864(16)32909-4/pdf	600 mg 1 times / day multiple, unknown dose: 600 mg route of administration: UNKNOWN experiment type: MULTIPLE co-administered:		PF-06747775 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
600 mg 1 times / day multiple, oral Highest studied dose Dose: 600 mg, 1 times / day Route: oral Route: multiple Dose: 600 mg, 1 times / day Sources: https://clinicaltrials.gov/ct2/show/results/NCT02349633	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://clinicaltrials.gov/ct2/show/results/NCT02349633	Other AEs: Anaemia, Ileus... Other AEs: Anaemia (serious, 25%) Ileus (serious, 25%) Pneumonia (serious, 25%) Pyrexia (serious, 25%) Dehydration (serious, 25%) Hyponatraemia (serious, 25%) Dyspnoea (serious, 25%) Dry eye (25%) Lacrimation increased (25%) Vision blurred (25%) Abdominal pain (50%) Diarrhoea (100%) Nausea (25%) Stomatitis (25%) Vomiting (25%) Mucosal inflammation (50%) Malaise (25%) Conjunctivitis (25%) Paronychia (50%) Rash pustular (25%) sinusitis (25%) Blood creatinine increased (50%) Blood urea increased (25%) Weight decreased (25%) Decreased appetite (25%) Hypokalaemi (50%) Headache (50%) Migraine (25%) Cough (25%) Dyspnoea (25%) Epistaxis (25%) Rhinorrhoea (25%) Dermatitis acneiform (25%) Dry skin (25%) Ingrowing nail (25%) Pruritus (25%) Flushing (25%) rash (50%) Sources: https://clinicaltrials.gov/ct2/show/results/NCT02349633

AEs

PubMed

Title	Date	PubMed
Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance.	2017-12-15	28526474
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.	2017-04-13	28287730
Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.	2016-04-12	27071706

Patents

Sample Use Guides

In Vivo Use Guide

PF-06747775 administered as continuous daily dosing in 21-day cycles. The starting dose of PF-06747775 25 mg daily.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:42:45 GMT 2025` Edited by `admin` on `Mon Mar 31 22:42:45 GMT 2025`
Record UNII	YXX2180047
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MAVELERTINIB

Official Name

English

EGFR T790M INHIBITOR PF-06747775

Preferred Name

English

N-((3R,4R)-4-FLUORO-1-(6-((3-METHOXY-1-METHYL-PYRAZOL-4-YL)AMINO)-9-METHYL-PURIN-2-YL)PYRROLIDIN-3-YL)PROP-2-ENAMIDE

Systematic Name

English

PF-06747775

Common Name

English

2-PROPENAMIDE, N-((3R,4R)-4-FLUORO-1-(6-((3-METHOXY-1-METHYL-1H-PYRAZOL-4-YL)AMINO)-9-METHYL-9H-PURIN-2-YL)-3-PYRROLIDINYL)-

Systematic Name

English

mavelertinib [INN]

Common Name

English

Mavelertinib [WHO-DD]

Common Name

English

MAVELERTINIB [USAN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C129825