Table 1 Anti-GPCR antibodies under clinical trials

From: Engineering therapeutic antibodies targeting G-protein–coupled receptors

Receptor target

Antibody drug

Disease indication

Company/institute

Status

CCR2

MNL1202

Bone metastases

Southwest Oncology group

Phase II

  

Arterial inflammation

Takeda

Phase II

  

Atherosclerosis

Millennium Pharmaceuticals

Phase II

CCR4

KW-0761 (Mogamulizumab)

Adult T-cell leukemia and lymphoma

Kyowa Hakko Kirin

Phase II

  

Peripheral T/NK-cell lymphoma

Kyowa Hakko Kirin

Phase II

  

Adult PTCL

Kyowa Hakko Kirin

Phase II

  

CTCL

Kyowa Hakko Kirin

Phase III

 

AMG761

Asthma

Amgen

Phase I

CCR5

PRO140

HIV infection

CytoDyn

Phase III

 

CCR5 mAb004

HIV infection

Human Genome Science

Phase I

 

HGS1025

Ulcerative colitis

Human Genome Science

Phase I

 

HGS004

HIV infection

Human Genome Science

Phase I

CCR9

MLN3126

Inflammation

Takeda

Phase I

CXCR4

BMS-936564

Multiple myeloma

Bristol-Myers Squibb

Phase I

 

ALX-0651

Stem cell mobilization

Ablynx

Phase I

 

LY-2624587

Metastatic cancer

Eli Lilly

Phase I

CXCR5

SAR113244

Systemic lupus erythematosus

Sanofi

Phase I

C5aR

NNC0151-0000-0000 (NN-8209)

Rheumatoid arthritis

Novo Nordisk

Phase II

 

NNC0215-0384 (NN-8210)

Rheumatoid arthritis, inflammation

Novo Nordisk

Phase I

CGRP-R

AMG-334

Migraine

Amgen

Phase II

  

Hot flashes

Amgen

Phase I

GCG-R

AMG-477

Type 2 diabetes

Amgen

Phase I

FZD1, 2, 5, 7, 8

OMP-18R5 (Vantictumab)

Solid tumor (NSCLC)

Oncomed

Phase I (combined with Docetaxel)

  

Metastatic breast cancer

Oncomed

Phase I (combined with paclitaxel)

  1. Abbreviations: CTCL, cutaneous T-cell lymphoma; GPCR, G-protein–coupled receptor; NK, natural killer; NSCLC, non-small-cell lung cancer; PTCL, peripheral T-cell lymphoma.