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. 2020 Nov 3;21(21):8240. doi: 10.3390/ijms21218240

Table 1.

Anti-GPCR antibodies approved by the US FDA or subject to clinical trial.

Antigen Type Antibody Screening Technology Drug Name Target Indication Status of Clinical Trial Reference
RAMP1-Fc, CGRPR-Fc Tg mouse immunization and hybridoma screening AimovigTM
(Erenumab)
CGRP receptor Migraine Approved [14]
CCR4-KLH Mouse immunization and hybridoma screening Poteligeo®
(Mogamulizumab)
CCR4 Refractory mycosis fungoides and Sézary disease Approved [15]
FZD7-Fc Synthetic human antibody phage library screening Vantictumab
(OMP-18R5)
FZD7 Non-small cell lung cancer, pancreatic cancer,
metastatic breast cancer
Phase I [16,17,18]
CCR5 expressing cells Mouse immunization and hybridoma screening Leronlimab
(Pro 140)
CCR5 HIV infection Phase III [19]
CCR2 expressing cells Mouse immunization and hybridoma screening Plozalizumab
(MLN-1202)
CCR2 Relapsing-remitting
multiple sclerosis
Phase II [20]
CXCR4 expressing cells Tg mouse immunization and phage library screening Ulocuplumab
(BMS-936564)
CXCR4 Acute myeloid leukemia Phase I/II [21]
C5Aa1 expressing cells Tg mouse immunization and hybridoma screening Avdoralimab
(IPH5401)
C5aR1 Non-small cell lung cancer, liver cancer Phase I [22]
Membrane fraction of GLP1R expressing cells Tg mouse immunization and hybridoma screening Glutazumab
(GMA102)
GLP1R Type 2
diabetes
Phase II [23]
Membrane fraction of GCGR expressing cells Tg mouse immunization and hybridoma screening Volagidemab
(REMD-477)
GCGR Diabetes mellitus Phase II [24]
Reconstituted
CNR1 GLB complex
Mouse immunization and hybridoma/phage library screening Namacizumab
(RYI-018)
CNR1 Non-alcoholic fatty
liver disease
Phase I [25]