Details of the Drug

General Information of Drug (ID: DMKM7EW)

Drug Name
PF-06463922
Synonyms SCHEMBL15274056
Indication
Disease Entry ICD 11 Status REF
Non-small-cell lung cancer 2C25.Y Phase 2 [1]
Solid tumour/cancer 2A00-2F9Z Phase 1/2 [2]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 406.4
Logarithm of the Partition Coefficient (xlogp) 1.5
Rotatable Bond Count (rotbonds) 0
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 7
Chemical Identifiers
Formula
C21H19FN6O2
IUPAC Name
(16R)-19-amino-13-fluoro-4,8,16-trimethyl-9-oxo-17-oxa-4,5,8,20-tetrazatetracyclo[16.3.1.02,6.010,15]docosa-1(22),2,5,10(15),11,13,18,20-octaene-3-carbonitrile
Canonical SMILES
C[C@@H]1C2=C(C=CC(=C2)F)C(=O)N(CC3=NN(C(=C3C4=CC(=C(N=C4)N)O1)C#N)C)C
InChI
InChI=1S/C21H19FN6O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12/h4-7,9,11H,10H2,1-3H3,(H2,24,25)/t11-/m1/s1
InChIKey
IIXWYSCJSQVBQM-LLVKDONJSA-N
Cross-matching ID
PubChem CID
71731823
ChEBI ID
CHEBI:143117
CAS Number
1454846-35-5
DrugBank ID
DB12130
TTD ID
D04DYC
ACDINA ID
D01222
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
ALK tyrosine kinase receptor (ALK) TTPMQSO ALK_HUMAN Inhibitor [3]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Non-small-cell lung cancer
ICD Disease Classification 2C25.Y
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
ALK tyrosine kinase receptor (ALK) DTT ALK 7.19E-15 0.18 0.61
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as PF-06463922
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Brigatinib DM7W94S Major Increased metabolism of PF-06463922 caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [4]
Lurbinectedin DMEFRTZ Major Decreased metabolism of PF-06463922 caused by Lurbinectedin mediated inhibition of CYP450 enzyme. Lung cancer [2C25] [5]
Pralsetinib DMWU0I2 Moderate Increased metabolism of PF-06463922 caused by Pralsetinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [6]
Selpercatinib DMZR15V Major Increased metabolism of PF-06463922 caused by Selpercatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [7]
Coadministration of a Drug Treating the Disease Different from PF-06463922 (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Gilteritinib DMTI0ZO Moderate Increased metabolism of PF-06463922 caused by Gilteritinib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [8]
Oliceridine DM6MDCF Major Increased metabolism of PF-06463922 caused by Oliceridine mediated induction of CYP450 enzyme. Acute pain [MG31] [9]
Erdafitinib DMI782S Major Increased metabolism of PF-06463922 caused by Erdafitinib mediated induction of CYP450 enzyme. Bladder cancer [2C94] [10]
Eslicarbazepine DMZREFQ Major Increased metabolism of PF-06463922 caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [11]
Bay 80-6946 DMLOS5R Moderate Increased metabolism of PF-06463922 caused by Bay 80-6946 mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [12]
Tazemetostat DMWP1BH Major Increased metabolism of PF-06463922 caused by Tazemetostat mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [13]
Ripretinib DM958QB Moderate Increased metabolism of PF-06463922 caused by Ripretinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [4]
Avapritinib DMK2GZX Major Increased metabolism of PF-06463922 caused by Avapritinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [7]
MK-1439 DM215WE Major Increased metabolism of PF-06463922 caused by MK-1439 mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [7]
Pemigatinib DM819JF Major Increased metabolism of PF-06463922 caused by Pemigatinib mediated induction of CYP450 enzyme. Liver cancer [2C12] [7]
Ubrogepant DM749I3 Moderate Increased metabolism of PF-06463922 caused by Ubrogepant mediated induction of CYP450 enzyme. Migraine [8A80] [14]
Rimegepant DMHOAUG Major Increased metabolism of PF-06463922 caused by Rimegepant mediated induction of CYP450 enzyme. Migraine [8A80] [15]
Siponimod DM2R86O Major Increased metabolism of PF-06463922 caused by Siponimod mediated induction of CYP450 enzyme. Multiple sclerosis [8A40] [4]
Fedratinib DM4ZBK6 Major Increased metabolism of PF-06463922 caused by Fedratinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [7]
Rucaparib DM9PVX8 Moderate Decreased metabolism of PF-06463922 caused by Rucaparib mediated inhibition of CYP450 enzyme. Ovarian cancer [2C73] [11]
Macimorelin DMQYJIR Moderate Increased metabolism of PF-06463922 caused by Macimorelin mediated induction of CYP450 enzyme. Pituitary gland disorder [5A60-5A61] [16]
Lefamulin DME6G97 Major Accelerated clearance of PF-06463922 due to the transporter induction by Lefamulin. Pneumonia [CA40] [17]
Darolutamide DMV7YFT Major Increased metabolism of PF-06463922 caused by Darolutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [18]
Upadacitinib DM32B5U Moderate Increased metabolism of PF-06463922 caused by Upadacitinib mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [19]
Voxelotor DMCS6M5 Major Increased metabolism of PF-06463922 caused by Voxelotor mediated induction of CYP450 enzyme. Sickle-cell disorder [3A51] [20]
Larotrectinib DM26CQR Moderate Increased metabolism of PF-06463922 caused by Larotrectinib mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [4]
Fluticasone DMGCSVF Moderate Increased metabolism of PF-06463922 caused by Fluticasone mediated induction of CYP450 enzyme. Vasomotor/allergic rhinitis [CA08] [11]
Betrixaban DM2C4RF Moderate Accelerated clearance of PF-06463922 due to the transporter induction by Betrixaban. Venous thromboembolism [BD72] [21]
⏷ Show the Full List of 23 DDI Information of This Drug

References

1 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2 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: 7476).
3 PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models. Cancer Cell. 2015 Jul 13;28(1):70-81.
4 Cerner Multum, Inc. "Australian Product Information.".
5 Product Information. Zepzelca (lurbinectedin). Jazz Pharmaceuticals, Palo Alto, CA.
6 Product Information. Gavreto (pralsetinib). Blueprint Medicines Corporation, Cambridge, MA.
7 Cerner Multum, Inc. "UK Summary of Product Characteristics.".
8 Product Information. Xospata (gilteritinib). Astellas Pharma US, Inc, Deerfield, IL.
9 Canadian Pharmacists Association.
10 Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
11 Product Information. Lorbrena (lorlatinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
12 Product Information. Aliqopa (copanlisib). Bayer Pharmaceutical Inc, West Haven, CT.
13 Product Information. Tazverik (tazemetostat). Epizyme, Inc, Cambridge, MA.
14 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
15 Product Information. Nurtec ODT (rimegepant). Biohaven Pharmaceuticals, New Haven, CT.
16 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
17 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
18 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
19 Product Information. Rinvoq (upadacitinib). AbbVie US LLC, North Chicago, IL.
20 Product Information. Oxbryta (voxelotor). Global Blood Therapeutics, Inc., South San Francisco, CA.
21 Gelosa P, Castiglioni L, Tenconi M, et.al "Pharmacokinetic drug interactions of the non-vitamin K antagonist oral anticoagulants (NOACs)" Pharmacol Res 135 (2018): 60-79. [PMID: 30040996]