MedKoo product information:

Canertinib

Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities. Canertinib binds to the intracellular domains of epidermal growth factor receptor tyrosine kinases (ErbB family), irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation. This agent also acts as a radiosensitizing agent and displays synergistic activity with other chemotherapeutic agents. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)

Current developer: Pfizer, Inc.

  1: Erlichman C, Boerner SA, Hallgren CG, Spieker R, Wang XY, James CD, Scheffer GL, Maliepaard M, Ross DD, Bible KC, Kaufmann SH. The HER tyrosine kinase inhibitor CI1033 enhances cytotoxicity of 7-ethyl-10-hydroxycamptothecin and topotecan by inhibiting breast cancer resistance protein-mediated drug efflux. Cancer Res. 2001 Jan 15;61(2):739-48. PubMed PMID: 11212277.

2: Rixe O, Franco SX, Yardley DA, Johnston SR, Martin M, Arun BK, Letrent SP, Rugo HS. A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer. Cancer Chemother Pharmacol. 2009 Nov;64(6):1139-48. Epub 2009 Mar 18. PubMed PMID: 19294387.

3: Dilworth JT, Wojtkowiak JW, Mathieu P, Tainsky MA, Reiners JJ Jr, Mattingly RR, Hancock CN. Suppression of proliferation of two independent NF1 malignant peripheral nerve sheath tumor cell lines by the pan-ErbB inhibitor CI-1033. Cancer Biol Ther. 2008 Dec;7(12):1938-46. Epub 2008 Dec 7. PubMed PMID: 18927496.

4: Jänne PA, von Pawel J, Cohen RB, Crino L, Butts CA, Olson SS, Eiseman IA, Chiappori AA, Yeap BY, Lenehan PF, Dasse K, Sheeran M, Bonomi PD. Multicenter, randomized, phase II trial of CI-1033, an irreversible pan-ERBB inhibitor, for previously treated advanced non small-cell lung cancer. J Clin Oncol. 2007 Sep 1;25(25):3936-44. PubMed PMID: 17761977.

5: Zinner RG, Nemunaitis J, Eiseman I, Shin HJ, Olson SC, Christensen J, Huang X, Lenehan PF, Donato NJ, Shin DM. Phase I clinical and pharmacodynamic evaluation of oral CI-1033 in patients with refractory cancer. Clin Cancer Res. 2007 May 15;13(10):3006-14. PubMed PMID: 17505003.

6: Chiappori AA, Ellis PM, Hamm JT, Bitran JD, Eiseman I, Lovalvo J, Burnett D, Olson S, Lenehan P, Zinner RG. A phase I evaluation of oral CI-1033 in combination with paclitaxel and carboplatin as first-line chemotherapy in patients with advanced non-small cell lung cancer. J Thorac Oncol. 2006 Nov;1(9):1010-9. PubMed PMID: 17409987.

7: Ako E, Yamashita Y, Ohira M, Yamazaki M, Hori T, Kubo N, Sawada T, Hirakawa K. The pan-erbB tyrosine kinase inhibitor CI-1033 inhibits human esophageal cancer cells in vitro and in vivo. Oncol Rep. 2007 Apr;17(4):887-93. PubMed PMID: 17342332.

8: Simon GR, Garrett CR, Olson SC, Langevin M, Eiseman IA, Mahany JJ, Williams CC, Lush R, Daud A, Munster P, Chiappori A, Fishman M, Bepler G, Lenehan PF, Sullivan DM. Increased bioavailability of intravenous versus oral CI-1033, a pan erbB tyrosine kinase inhibitor: results of a phase I pharmacokinetic study. Clin Cancer Res. 2006 Aug 1;12(15):4645-51. PubMed PMID: 16899614.

9: Garland LL, Hidalgo M, Mendelson DS, Ryan DP, Arun BK, Lovalvo JL, Eiseman IA, Olson SC, Lenehan PF, Eder JP. A phase I clinical and pharmacokinetic study of oral CI-1033 in combination with docetaxel in patients with advanced solid tumors. Clin Cancer Res. 2006 Jul 15;12(14 Pt 1):4274-82. PubMed PMID: 16857802.

10: Dorow DS, Cullinane C, Conus N, Roselt P, Binns D, McCarthy TJ, McArthur GA, Hicks RJ. Multi-tracer small animal PET imaging of the tumour response to the novel pan-Erb-B inhibitor CI-1033. Eur J Nucl Med Mol Imaging. 2006 Apr;33(4):441-52. Epub 2006 Feb 1. PubMed PMID: 16450138.

11: Skvortsov S, Skvortsova I, Sarg B, Loeffler-Ragg J, Lindner H, Lukas P, Tabernero J, Zwierzina H. Irreversible pan-ErbB tyrosine kinase inhibitor CI-1033 induces caspase-independent apoptosis in colorectal cancer DiFi cell line. Apoptosis. 2005 Oct;10(5):1175-86. PubMed PMID: 16151650.

12: Campos S, Hamid O, Seiden MV, Oza A, Plante M, Potkul RK, Lenehan PF, Kaldjian EP, Varterasian ML, Jordan C, Charbonneau C, Hirte H. Multicenter, randomized phase II trial of oral CI-1033 for previously treated advanced ovarian cancer. J Clin Oncol. 2005 Aug 20;23(24):5597-604. PubMed PMID: 16110019.

13: Hughes DP, Thomas DG, Giordano TJ, McDonagh KT, Baker LH. Essential erbB family phosphorylation in osteosarcoma as a target for CI-1033 inhibition. Pediatr Blood Cancer. 2006 May 1;46(5):614-23. PubMed PMID: 16007579.

14: Nemunaitis J, Eiseman I, Cunningham C, Senzer N, Williams A, Lenehan PF, Olson SC, Bycott P, Schlicht M, Zentgraff R, Shin DM, Zinner RG. Phase 1 clinical and pharmacokinetics evaluation of oral CI-1033 in patients with refractory cancer. Clin Cancer Res. 2005 May 15;11(10):3846-53. PubMed PMID: 15897585.

15: Dewji MR. Early phase I data on an irreversible pan-erb inhibitor: CI-1033. What did we learn? J Chemother. 2004 Nov;16 Suppl 4:44-8. Review. PubMed PMID: 15688609.

16: Calvo E, Tolcher AW, Hammond LA, Patnaik A, de Bono JS, Eiseman IA, Olson SC, Lenehan PF, McCreery H, Lorusso P, Rowinsky EK. Administration of CI-1033, an irreversible pan-erbB tyrosine kinase inhibitor, is feasible on a 7-day on, 7-day off schedule: a phase I pharmacokinetic and food effect study. Clin Cancer Res. 2004 Nov 1;10(21):7112-20. PubMed PMID: 15534081.

17: Murakami M, Sasaki T, Yamasaki S, Kuwahara K, Miyata H, Chayama K. Induction of apoptosis by ionizing radiation and CI-1033 in HuCCT-1 cells. Biochem Biophys Res Commun. 2004 Jun 18;319(1):114-9. PubMed PMID: 15158449.

18: Nyati MK, Maheshwari D, Hanasoge S, Sreekumar A, Rynkiewicz SD, Chinnaiyan AM, Leopold WR, Ethier SP, Lawrence TS. Radiosensitization by pan ErbB inhibitor CI-1033 in vitro and in vivo. Clin Cancer Res. 2004 Jan 15;10(2):691-700. PubMed PMID: 14760092.

19: Harari PM, Huang SM. Searching for reliable epidermal growth factor receptor response predictors: commentary re M. K. Nyati et al., Radiosensitization by pan-ErbB inhibitor CI-1033 in vitro and in vivo. Clin. Cancer Res., 10: 691-700, 2004. Clin Cancer Res. 2004 Jan 15;10(2):428-32. Review. PubMed PMID: 14760061.

20: Allen LF, Eiseman IA, Fry DW, Lenehan PF. CI-1033, an irreversible pan-erbB receptor inhibitor and its potential application for the treatment of breast cancer. Semin Oncol. 2003 Oct;30(5 Suppl 16):65-78. Review. PubMed PMID: 14613028.

21: Allen LF, Lenehan PF, Eiseman IA, Elliott WL, Fry DW. Potential benefits of the irreversible pan-erbB inhibitor, CI-1033, in the treatment of breast cancer. Semin Oncol. 2002 Jun;29(3 Suppl 11):11-21. Review. PubMed PMID: 12138393.

22: Slichenmyer WJ, Elliott WL, Fry DW. CI-1033, a pan-erbB tyrosine kinase inhibitor. Semin Oncol. 2001 Oct;28(5 Suppl 16):80-5. Review. PubMed PMID: 11706399.

23: Gieseg MA, de Bock C, Ferguson LR, Denny WA. Evidence for epidermal growth factor receptor-enhanced chemosensitivity in combinations of cisplatin and the new irreversible tyrosine kinase inhibitor CI-1033. Anticancer Drugs. 2001 Sep;12(8):683-90. PubMed PMID: 11604556.