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Details

Stereochemistry ABSOLUTE
Molecular Formula C17H15N9
Molecular Weight 345.3613
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of SAVOLITINIB

SMILES

C[C@H](N1N=NC2=NC=C(N=C12)C3=CN(C)N=C3)C4=CN5C=CN=C5C=C4

InChI

InChIKey=XYDNMOZJKOGZLS-NSHDSACASA-N
InChI=1S/C17H15N9/c1-11(12-3-4-15-18-5-6-25(15)10-12)26-17-16(22-23-26)19-8-14(21-17)13-7-20-24(2)9-13/h3-11H,1-2H3/t11-/m0/s1

HIDE SMILES / InChI

Molecular Formula C17H15N9
Molecular Weight 345.3613
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including http://www.chi-med.com/initiation-of-azd6094-hmpl-504volitinib-global-phase-ii-study-in-papillary-renal-cell-carcinoma-2/

Savolitinib (AZD6094, HMPL-504) has been demonstrated to inhibit the growth of tumors in a series of preclinical disease models, selectively for those tumors with aberrant c-Met signaling. Phase I dose escalation studies were initiated in Australia and China in 2012 and 2013 respectively. Savolitinib has demonstrated good safety and tolerability and favorable pharmacokinetic properties in late stage cancer patients, and has shown encouraging anti-tumor activity in several tumor-types, in particular for metastatic Papillary Renal Cell Cancer (PRCC). Phase II, study designed to evaluate the efficacy and safety of savolitinib in patients with locally advanced or metastatic PRCC. Approximately 20 centers in the United States, Canada, and Europe will participate in the study. The primary objective of this study is to assess the anti-tumor activity in patients with PRCC as measured by overall response rate according to Response Evaluation Criteria in Solid Tumours (“RECIST”). The secondary objectives for this study are to: assess the progression free survival and duration of response in patients with PRCC according to RECIST; assess the safety and tolerability in the treatment of patients with PRCC; characterize the pharmacokinetics and pharmacodynamics of savolitinib and metabolites following administration to steady state after multiple dosing when given orally.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
likely [IC50 100 uM]
likely [IC50 100 uM]
no
no
no
no
no
weak [EC50 >3.6 uM]
weak [IC50 35 uM]
weak [IC50 50 uM]
weak [IC50 >30 uM]
weak [IC50 >50 uM]
weak [IC50 >50 uM]
weak [IC50 >50 uM]
weak [IC50 >50 uM]
weak [IC50 >50 uM]
weak [IC50 >50 uM]
weak
yes [IC50 11 uM]
yes [IC50 11 uM]
yes [IC50 13 uM]
yes [IC50 16 uM]
yes [IC50 20 uM]
yes [IC50 22 uM]
yes [IC50 24 uM]
yes [IC50 27 uM]
yes [IC50 4.7 uM]
yes [IC50 6.4 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
major
major
major
major
major
minor
yes (co-administration study)
Comment: Rifampicin decreased Cmax and AUC by 37% and 49%.
minor
yes (co-administration study)
Comment: Rifampicin decrease Cmax and AUC by 55% and 61%.
no
yes
no (co-administration study)
Comment: Itraconazole increased Cmax and AUC by 5.2% and 8.4%.
Tox targets

Tox targets

PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

600 mg by mouth once daily
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: In vitro, savolitinib inhibits MET phosphorylation with nanomolar potency, which correlates with blockade of PI3K/AKT and MAPK signaling as well as MYC down-regulation.
Unknown
Substance Class Chemical
Created
by admin
on Sat Dec 16 08:47:02 GMT 2023
Edited
by admin
on Sat Dec 16 08:47:02 GMT 2023
Record UNII
2A2DA6857R
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SAVOLITINIB
INN   USAN   WHO-DD  
USAN   INN  
Official Name English
VOLITINIB
WHO-DD  
Common Name English
HMPL-504
Code English
1-((S)-1-(IMIDAZO(1,2-A)PYRIDIN-6-YL)ETHYL)-6-(1-METHYL-1H-PYRAZOL-4-YL)-1H-(1,2,3)-TRIAZOLO(4,5-B)PYRAZINE
Systematic Name English
AZD6094
Code English
SAVOLITINIB [USAN]
Common Name English
1H-1,2,3-TRIAZOLO(4,5-B)PYRAZINE, 1-((1S)-1-IMIDAZO(1,2-A)PYRIDIN-6-YLETHYL)-6-(1-METHYL-1H-PYRAZOL-4-YL)-
Systematic Name English
Savolitinib [WHO-DD]
Common Name English
savolitinib [INN]
Common Name English
AZD-6094
Code English
Classification Tree Code System Code
NCI_THESAURUS C129825
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
NCI_THESAURUS C1967
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
NCI_THESAURUS C1742
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
Code System Code Type Description
NCI_THESAURUS
C104732
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
USAN
EF-02
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
EVMPD
SUB181945
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
CAS
1313725-88-0
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
EPA CompTox
DTXSID801111016
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
PUBCHEM
68289010
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
DRUG BANK
DB12048
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
SMS_ID
100000168519
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
INN
9935
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
FDA UNII
2A2DA6857R
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
ChEMBL
CHEMBL3545336
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
WIKIPEDIA
Savolitinib
Created by admin on Sat Dec 16 08:47:02 GMT 2023 , Edited by admin on Sat Dec 16 08:47:02 GMT 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Related Record Type Details
ACTIVE MOIETY