Skip to main content
. 2023 Feb 17;15(4):1287. doi: 10.3390/cancers15041287

Table 2.

Literature of IGF-1R inhibitors under clinical investigation in PCa.

Agents Property Phase/Region Population Treatment Schemes Key Activity Data Safety and Adverse Events References
Cixutumumab Recombinant human mAb, IgG1, targets IGF-1R Phase II (2015/2020/USA) 210 patients with mHSPC (PSA ≥ 5 ng/mL) Cixutumumab (10 mg/kg, intravenously, 2 times/28 d, last 28 w) + Bicalutamide (oral, daily) + LHRH agonist

  1. Increase the undetectable PSA (≤0.2 ng/mL) ratio, but not improve overall survival

  1. Well tolerated;

  2. Minimal increase in adverse events such as hyperglycemia.

 [90,99]
(J Clin Oncol, 2015); (Prostate Cancer and Prostatic Diseases, 2020)
Phase I
(2019/USA)		 16 patients with mCRPC (PSA ≥ 2 ng/mL) Cixutumumab (6 mg/kg, 12 w) + Temsirolimus

  1. Limited antitumor effect with no PSA decreases ≥ 50%.

  1. Hyperglycemia (grade ≤ 3);

  2. No grade 4 events or deaths occurred.

 [98]
(Clinical Genitourinary Cancer, 2020)
Phase II
(2015/USA) 		132 patients with docetaxel-treated mCRPC (PSA ≥ 2 ng/mL) Cixutumumab (6 mg/kg, intravenously,3 times/21 d) + Mitoxantrone + Prednisone

  1. A PSA decline of ≥ 50% from baseline occurred in 18.5% of patients;

  2. The median cPFS was 4.1 months and median OS was 10.8 months.

  1. Safety in the mass;

  2. Fatigue and weight decreased mildly.

 [100]
(Eur J Cancer, 2015)
Figitumumab Full human mAb, IgG2, blocks IGF-1 binds to IGF-1R Phase II
(2012/Canada)		 16 patients with localized PCa (PSA ≥ 10 ng/mL) Figitumumab (20 mg/kg, intravenously every 3 weeks, 3 cycles)

  1. Decline serum PSA and testosterone levels; inhibit androgen receptor expression.

  1. Mild adverse events (grade ≤ 3).

 [102]
(Clin Cancer Res, 2012)
Phase II
(2014/UK)		 204 patients with mCRPC Figitumumab (10 or 20 mg/kg, intravenously, 12 m) + Docetaxel vs. Docetaxel alone

  1. Higher stable PSA response rate (31% vs. 21%)

  2. Shorter median PFS (4.9 months vs. 7.9 months).

  1. More treatment-related serious adverse events (41% vs. 15%);

  2. Hyperglycemia, diarrhea, asthenia.

 [101]
(Clin Cancer Res, 2014)

Abbreviations: mAb, monoclonal antibody; OS, overall survival; PFS, progression-free survival; d, days; w, weeks; m, months; PSA, prostate-specific antigen; mHSPC, metastatic castration-sensitive prostate cancer; CRPC, castration-resistant prostate cancer.