Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT731LW)

• DTT Name: Colony stimulating factor-1 receptor (CSF-1R)
• Synonyms: Macrophage colony-stimulating factor 1 receptor
• Gene Name: CSF1R
• DTT Type: Clinical trial target; [1]
• UniProt ID: E9PEK4_HUMAN
• TTD ID: T01110
• Sequence:
  MGPGVLLLLLVATAWHGQGIPVIEPSVPELVVKPGATVTLRCVGNGSVEWDGPPSPHWTL
  YSDGSSSILSTNNATFQNTGTYRCTEPGDPLGGSAAIHLYVKDPARPWNVLAQEVVVFED
  QDALLPCLLTDPVLEAGVSLVRVRGRPLMRHTNYSFSPWHGFTIHRAKFIQSQDYQCSAL
  MGGRKVMSISIRLKVQKVIPGPPALTLVPAELVRIRGEAAQIVCSASSVDVNFDVFLQHN
  NTKLAIPQQSDFHNNRYQKVLTLNLDQVDFQHAGNYSCVASNVQGKHSTSMFFRVVESAY
  LNLSSEQNLIQEVTVGEGLNLKVMVEAYPGLQGFNWTYLGPFSDHQPEPKLANATTKDTY
  RHTFTLSLPRLKPSEAGRYSFLARNPGGWRALTFELTLRYPPEVSVIWTFINGSGTLLCA
  ASGYPQPNVTWLQCSGHTDRCDEAQVLQVWDDPYPEVLSQEPFHKVTVQSLLTVETLEHN
  QTYECRAHNSVGSGSWAFIPISAGAHTHPPDEFLFTPVVVACMSIMALLLLLLLLLLYKY
  KQKPKYQVRWKIIESYEGNSYTFIDPTQLPYNEKWEFPRNNLQFGKTLGAGAFGKVVEAT
  AFGLGKEDAVLKVAVKMLKSTAHADEKEALMSELKIMSHLGQHENIVNLLGACTHGGTVA
  SPARVWTPMWR
• Function: A cytokine which controls the production, differentiation, and function of macrophages.

Molecular Interaction Atlas (MIA) of This DTT

8 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ARRY-382	DM0VGDC	Solid tumour/cancer	2A00-2F9Z	Phase 2	[2]
JNJ-40346527	DM219SF	Hodgkin lymphoma	2B30	Phase 2	[3]
MCS-110	DM0CL4I	Bone metastases	2D50	Phase 2	[1]
PD-360324	DM6F5EV	Rheumatoid arthritis	FA20	Phase 2	[4]
RG7155	DM8JMNL	Solid tumour/cancer	2A00-2F9Z	Phase 2	[5]
FPA-008	DM3ZN6Y	Autoimmune diabetes	5A10	Phase 1/2	[6]
AMG 820	DMB6Q19	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]
IMC-CS4	DMUYN26	Solid tumour/cancer	2A00-2F9Z	Phase 1	[1]

References

• [1] Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
• [2] Company report (Array)
• [3] An Open-Label, Multicenter, Phase I/II Study of JNJ-40346527, a CSF-1R Inhibitor, in Patients with Relapsed or Refractory Hodgkin Lymphoma. Clin Cancer Res. 2015 Apr 15;21(8):1843-50.
• [4] Monoclonal antibody against macrophage colony-stimulating factor suppresses circulating monocytes and tissue macrophage function but does not alter cell infiltration/activation in cutaneous lesions or clinical outcomes in patients with cutaneous lupus erythematosus.Clin Exp Immunol.2016 Feb;183(2):258-70.
• [5] Targeting tumor-associated macrophages with anti-CSF-1R antibody reveals a strategy for cancer therapy. Cancer Cell. 2014 Jun 16;25(6):846-59.
• [6] Company report (Five Prime Therapeutics)