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. 2016 Sep 19;8(1):1814–1844. doi: 10.18632/oncotarget.12123

Table 1. Inhibitors of IGF-IR that underwent pre-clinical evaluation.

Inhibitor Phase Tumor Type Manufacturer Type of inhibitor References
A-928605 Pre-clinical Neuroblastoma Abbott Dual IGF-IR/IR tyrosine kinase inhibitor [283]
ABDP Pre-clinical Colon cancer AstraZeneca Dual IGF-IR/IR tyrosine kinase inhibitor [284]
AG-1024 Pre-clinical Breast cancer, colorectal cancer, glioma, hepatocellular carcinoma, mesothelioma, NSCLC, osteosarcoma, pancreatic cancer, prostate cancer Calbiochem EMD Biosciences Tyrosine kinase and autophosphorylation inhibitor [268, 285–294]
BMS-536924 Pre-clinical AML, breast cancer, ovarian cancer Bristol-Myers Squibb ATP-competitive inhibitor [59, 249, 295]
BMS-554417 Pre-clinical Breast cancer, ovarian cancer Bristol-Myers Squibb Reversible ATP-competitive small molecule inhibitor [153]
GSK1838705A Pre-clinical Breast cancer, cervical cancer, colon cancer, Ewing sarcoma, glioma, head and neck cancer, hepatocellular carcinoma, lung cancer, NPM-ALK+ T-cell lymphoma, ovarian cancer, PCM, pancreatic cancer, prostate cancer GlaxoSmithKline Triple IGF-IR/IR/ALK tyrosine kinase inhibitor [177, 296–298]
GSK1904529A Pre-clinical Askin tumor, breast cancer, cervical cancer, colon cancer, Ewing sarcoma, head and neck cancer, lung cancer, NPM-ALK+ T-cell lymphoma, ovarian cancer, PCM, prostate cancer GlaxoSmithKline Dual IGF-IR/IR tyrosine kinase inhibitor [299]
INSM-18 Pre-clinical Prostate cancer Insmed Dual IGF-IR/HER2 small molecule inhibitor [300]
NVP-ADW742 Pre-clinical AML, Ewing sarcoma, medulloblastoma, NSCLC Novartis Reversible ATP-competitive small molecule inhibitor [60, 257, 259, 301, 302]
NVP-AEW541 Pre-clinical AML, breast cancer, colon cancer, endometrial cancer, esophageal cancer, Ewing sarcoma, gastric cancer, gastrointestinal stromal tumors, glioma, head and neck cancer, hepatocellular carcinoma, medulloblastoma, neuroblastoma, ovarian cancer, pancreatic cancer, PCM, pituitary tumors, prostate cancer, soft tissue sarcomas, synovial sarcoma Novartis Reversible ATP-competitive small molecule inhibitor [56, 57, 61, 218–240]
Picropodophyllin (PPP; AXL1717) Pre-clinical Breast cancer, CML, colon cancer, Ewing sarcoma, glioblastoma, hepatocellular carcinoma, lung cancer, MCL, medulloblastoma, neuroblastoma, NPM-ALK+ T-cell lymphoma, osteosarcoma, ovarian cancer, pancreatic cancer, PCM, uveal melanoma Axelar Non-ATP-competitive small molecule inhibitor [21–23, 56, 64, 203–216]