U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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 of MAVELERTINIB

SMILES

COC1=NN(C)C=C1NC2=NC(=NC3=C2N=CN3C)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

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

Curator's Comment: # Pfizer

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P00533|||Q9GZX1
Gene ID: 1956.0
Gene Symbol: EGFR
Target Organism: Homo sapiens (Human)
3.0 nM [IC50]
307.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
0.28 h
1 mg/kg single, intravenous
dose: 1 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PF-06747775 plasma
Rattus norvegicus
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
22%
1 mg/kg single, intravenous
dose: 1 mg/kg
route of administration: Intravenous
experiment type: SINGLE
co-administered:
PF-06747775 plasma
Rattus norvegicus
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Other AEs: Dermatitis acneiform, Lacrimation increased...
Other AEs:
Dermatitis acneiform (25%)
Lacrimation increased (25%)
Paronychia (50%)
Vision blurred (25%)
Migraine (25%)
Rash pustular (25%)
Ileus (serious, 25%)
sinusitis (25%)
Abdominal pain (50%)
Diarrhoea (100%)
Pyrexia (serious, 25%)
Dry skin (25%)
Cough (25%)
Nausea (25%)
Blood creatinine increased (50%)
Stomatitis (25%)
Pneumonia (serious, 25%)
Dehydration (serious, 25%)
Blood urea increased (25%)
Vomiting (25%)
Hyponatraemia (serious, 25%)
Ingrowing nail (25%)
Weight decreased (25%)
Dyspnoea (serious, 25%)
Mucosal inflammation (50%)
Anaemia (serious, 25%)
Dry eye (25%)
Malaise (25%)
Decreased appetite (25%)
Pruritus (25%)
Conjunctivitis (25%)
Dyspnoea (25%)
Hypokalaemi (50%)
Epistaxis (25%)
Headache (50%)
Flushing (25%)
Rhinorrhoea (25%)
rash (50%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Diarrhoea 100%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Blood urea increased 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Conjunctivitis 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Cough 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Decreased appetite 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dermatitis acneiform 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dry eye 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dry skin 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dyspnoea 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Epistaxis 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Flushing 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Ingrowing nail 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Lacrimation increased 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Malaise 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Migraine 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Nausea 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Pruritus 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Rash pustular 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Rhinorrhoea 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Stomatitis 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Vision blurred 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Vomiting 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Weight decreased 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
sinusitis 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Abdominal pain 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Blood creatinine increased 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Headache 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Hypokalaemi 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Mucosal inflammation 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Paronychia 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
rash 50%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Anaemia serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dehydration serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Dyspnoea serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Hyponatraemia serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Ileus serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Pneumonia serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
Pyrexia serious, 25%
600 mg 1 times / day multiple, oral (unknown)
Highest studied dose
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
unhealthy, ADULT
n = 4
Health Status: unhealthy
Condition: Non-small cell lung cancer
Age Group: ADULT
Sex: M+F
Food Status: UNKNOWN
Population Size: 4
Sources:
PubMed

PubMed

TitleDatePubMed
Patents

Patents

Sample Use Guides

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 Sat Dec 16 09:32:38 UTC 2023
Edited
by admin
on Sat Dec 16 09:32:38 UTC 2023
Record UNII
YXX2180047
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MAVELERTINIB
INN   USAN  
Official 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
EGFR T790M INHIBITOR PF-06747775
Common Name English
Mavelertinib [WHO-DD]
Common Name English
MAVELERTINIB [USAN]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
NCI_THESAURUS C2167
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
Code System Code Type Description
NCI_THESAURUS
C120307
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
SMS_ID
100000177314
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
CAS
1776112-90-3
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
INN
10660
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
PUBCHEM
91668194
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
FDA UNII
YXX2180047
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
USAN
DE-167
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
EVMPD
SUB192567
Created by admin on Sat Dec 16 09:32:38 UTC 2023 , Edited by admin on Sat Dec 16 09:32:38 UTC 2023
PRIMARY
Related Record Type Details
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