Table 2.

Clinical evaluation of small-molecule IGF-IR inhibitors in cancer patients

Drug	Combination	Cancer type	Phase	Participants	Response	Ref. or trial ID
Linsitinib (OSI-906)	None	Locally advanced or metastatic adrenocortical carcinoma	3	139	OS, 323 days (95% CI 256–507) for linsitinib, 356 days (95% CI 249–556) for placebo	[158] NCT00924989
Linsitinib	None	Recurrent small cell lung cancer	2	44	SD, 3.45%; PFS, 1.2 months (95% CI 1.1–1.4); OS, 3.4 months (95% CI 1.8–5.6). The response to linsitinib is inferior to topotecan.	[159] NCT01533181
Linsitinib	Everolimus	Refractory metastatic colorectal cancer	1	18	No objective responses to treatment. PFS, 8 weeks (95% CI 7–9); OS, 30.6 weeks (95% CI 16.7–32.1)	[160] NCT01154335
Linsitinib	None	Metastatic prostate cancer	2	17	PSA partial response, 5.88%; PR, 10%; SD,80%; PD, 10%; PFS, 4.7 months (95% CI 3–6.7)	[161] NCT01533246
Linsitinib	Erlotinib	Advanced non-small cell lung cancer	2	88	Combination of linsitinib with erlotinib resulted in an increase in the incidence of renal and hepatic toxicities compared to erlotinib alone. Combination of linsitinib with erlotinib did not improve the PFS and OS compared to erlotinib alone.	NCT01221077
Linsitinib	None	Gastrointestinal stromal tumors	2	20	CR + PR + SD (≥ 9 months), 40%; PFS rate at 9 months, 52%; OS rate at 9 months, 80%	[162] NCT01560260
AXL1717	None	Recurrent or progressive malignant astrocytoma	1	9	Tumor response rate, 44%; SD for 12 months, 22.2%	[163] NCT00562380

CR complete response; OS overall survival, PD progressive disease, PFS progression-free survival, PR partial response, SD stable disease, Trial ID registered number at ClinicalTrials.gov