Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMMHSLC)

Drug Name
Afq056 Drug Info
Synonyms Mavoglurant
Indication
Disease Entry ICD 11 Status REF
Fragile X syndrome LD55 Phase 2/3 [1] , [2]
Cross-matching ID
PubChem CID
9926832
CAS Number
CAS 543906-09-8
TTD Drug ID
DMMHSLC
INTEDE Drug ID
DR1870

Molecule(s) Related to This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Metabotropic glutamate receptor 5 (mGluR5) TTHS256 GRM5_HUMAN Modulator [3]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID Highest Status REF
Cytochrome P450 1A1 (CYP1A1) DE6OQ3W CP1A1_HUMAN Phase 2/3 [4]

The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule Molecule Type Gene Name Liver Colon Kidney Small Intestine
Metabotropic glutamate receptor 5 (mGluR5) DTT GRM5 3.621 1.888 3.567 4.318
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 5.952 6.384 4.897 6.293
Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

The Studied Disease Fragile X syndrome
ICD Disease Classification LD55
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Metabotropic glutamate receptor 5 (mGluR5) DTT GRM5 9.81E-07 -0.26 -0.54
Cytochrome P450 1A1 (CYP1A1) DME CYP1A1 6.83E-06 -1.42E-01 -4.93E-01
Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7586).
2 ClinicalTrials.gov (NCT01433354) Long-term, Safety and Tolerability Study of AFQ056 in Adolescent Patients With Fragile X Syndrome (Open-label). U.S. National Institutes of Health.
3 Metabolism and disposition of the metabotropic glutamate receptor 5 antagonist (mGluR5) mavoglurant (AFQ056) in healthy subjects. Drug Metab Dispos. 2013 Sep;41(9):1626-41.
4 Methods to Assess Pulmonary Metabolism.