Table 3.

Anti GPCRs drugs and antibodies under clinical trials [48].

Cancer	Inhibitor	Type of molecule	Receptor	Phase	Sponsor
Prostate cancer	Zibotentan (ZD4054) Atrasentan (ABT-627)	Small molecule Small molecule	Endothelin A receptor Endothelin A receptor	Phase I, II, III Phase II, Phase III (combine with docetaxel and prednisone)	AstraZeneca Abbott Southwest Oncology Group
Head and neck cancer	GDC-0449 (Vismodegib)	Small molecule	Smoothened receptor (SMO)	Phase II	Sue Yom in collaboration with Genentech, Inc
Ovarian cancer	GDC-0449 (Vismodegib) Propranolol (beta-blockers)	Small molecule Small molecule	Endothelin Receptor beta-adrenergic receptor	Phase II Phase I	Genentech, Inc. Washington University School of Medicine
Pancreatic cancer	CCX872 (OMP-18R5) Vantictumab G17DT	Small molecule Antibodies Immunogen	CCR2 Frizzled receptor FZD7 Cholecystokinin-2 receptor	Phase I Phase I (combine with nab-paclitaxel and gemcitabine) Phase III	ChemoCentryx OncoMed Pharmaceuticals, Inc. Cancer Advances Inc
Multiple myeloma	BMS-936564	Antibodies	CXCR4	Phase I	Bristol-Myers Squibb
Melanoma	Plozalizumab	Humanized monoclonal antibody	CCR2	phase I	Millennium Pharmaceuticals, Inc.
Adult T-cell leukemia and lymphoma	KW-0761 (Mogamulizumab)	Antibodies	CCR4	Phase II	Kyowa Hakko Kirin
Metastatic breast cancer	OMP-18R5 (Vantictumab) beta-blockers	Antibodies Small molecule	FZD1, 2, 5, 7, 8 beta-adrenergic receptor	Phase I (combined with paclitaxel) Phase II	OncoMed Pharmaceuticals, Inc. Columbia University
Non-small cell lung carcinoma	OMP-18R5 (Vantictumab)	Antibodies	Frizzled receptors (FZD1, 2, 5, 7, 8)	Phase I (combined with docetaxel)	OncoMed Pharmaceuticals, Inc.
Advanced solid tumors	AAT-007	Small molecule	Prostaglandin E2 receptor 4 (EP4)	Phase II	University of Maryland
Advanced or metastatic cancer	LY-2624587	Antibodies	CXCR4	Phase I	Eli Lilly and Company