Details of the Drug

General Information of Drug (ID: DMC2IJN)

• Drug Name: TPX-0022
• Synonyms: CSF1R-IN-2; SCHEMBL20694441; TPX0022; NSC820832; NSC-820832; HY-111787; CS-0091874; 2271119-26-5

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 409.4
  Logarithm of the Partition Coefficient (xlogp); 2.1
  Rotatable Bond Count (rotbonds); 1
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 8
• Chemical Identifiers:
  Formula: C20H20FN7O2
  IUPAC Name: (11S)-16-amino-2-ethyl-6-fluoro-11-methyl-14-oxo-10-oxa-2,13,17,18,21-pentazatetracyclo[13.5.2.04,9.018,22]docosa-1(21),4(9),5,7,15(22),16,19-heptaene-5-carbonitrile
  Canonical SMILES: CCN1CC2=C(C=CC(=C2C#N)F)O[C@H](CNC(=O)C3=C4N=C1C=CN4N=C3N)C
  InChI: InChI=1S/C20H20FN7O2/c1-3-27-10-13-12(8-22)14(21)4-5-15(13)30-11(2)9-24-20(29)17-18(23)26-28-7-6-16(27)25-19(17)28/h4-7,11H,3,9-10H2,1-2H3,(H2,23,26)(H,24,29)/t11-/m0/s1
  InChIKey: UUDPUQDMSHQSKH-NSHDSACASA-N
• Cross-matching ID:
  PubChem CID: 137455315
  TTD ID: D7M8LI

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Macrophage colony-stimulating factor 1 receptor (CSF1R)	TT7MRDV	CSF1R_HUMAN	Inhibitor	[2]
Proto-oncogene c-Met (MET)	TTNDSF4	MET_HUMAN	Inhibitor	[2]
Proto-oncogene c-Src (SRC)	TT6PKBN	SRC_HUMAN	Inhibitor	[2]

Molecular Expression Atlas of This Drug

• The Studied Disease: Solid tumour/cancer
• ICD Disease Classification: 2A00-2F9Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Proto-oncogene c-Met (MET)	DTT	MET	1.08E-03	-0.24	-0.4

References

• [1] ClinicalTrials.gov (NCT03993873) Phase 1 Study of TPX-0022, a MET/CSF1R/SRC Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in MET. U.S. National Institutes of Health.
• [2] Clinical pipeline report, company report or official report of Turning Point Therapeutics.