Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer agents in preclinical trials

Anticancer molecular libraries

MedKoo product information:

Momelotinib (AZD-8931)

Description of Momelotinib (AZD8931):  Momelotinib is an erbB receptor tyrosine kinase inhibitor with potential antineoplastic activity. erbB kinase inhibitor AZD8931 binds to and inhibits erbB tyrosine receptor kinases, which may result in the inhibition of cellular proliferation and angiogenesis in tumors expressing erbB. The erbB protein family, also called the epidermal growth factor receptor (EGFR) family, plays major roles in tumor cell proliferation and tumor vascularization. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:   AstraZeneca.

Recent study showed that AZD8931 has a unique pharmacologic profile providing equipotent inhibition of EGFR, erbB2, and erbB3 signaling and showing greater antitumor activity than agents with a narrower spectrum of erbB receptor inhibition in specific preclinical models. AZD8931 provides the opportunity to investigate whether simultaneous inhibition of erbB receptor signaling could be of utility in the clinic, particularly in the majority of solid tumors that do not overexpress erbB2 (Source: Clin Cancer Res. 2010 Feb 15;16(4):1159-69.) 

1: Hickinson DM, Klinowska T, Speake G, Vincent J, Trigwell C, Anderton J, Beck S, Marshall G, Davenport S, Callis R, Mills E, Grosios K, Smith P, Barlaam B, Wilkinson RW, Ogilvie D. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010 Feb 15;16(4):1159-69. Epub 2010 Feb 9. PubMed PMID: 20145185.

2:  Bradbury, Robert Hugh; Hennequin, Laurent Francois Andre; Barlaam, Bernard Christophe. Preparation of quinazoline derivatives as EGFR tyrosine kinase inhibitors. PCT Int. Appl. (2005), 84 pp. CODEN: PIXXD2 WO 2005028469 A1 20050331 CAN 142:355277 AN 2005:283486 CAPLUS

3: Iacona, Lisa Renee Bailey; Smith, Ian; Stuart, Mary. Combination comprising 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[[1-(N-methylcarbamoylmethyl) piperidin-4-yl]oxy]quinazoline for breast cancer treatment. PCT Int. Appl. (2009), 75pp. CODEN: PIXXD2 WO 2009138779 A1 20091119 CAN 152:20025 AN 2009:1432983 CAPLUS

4: Boardman, Kay Alison; Burns, Susan Elizabeth; Dobson, Andrew Hornby; Whitlock, Brian. Preparation of fumarate salt of 4-(3-chloro-2-fluoroanilino)-7-methoxy-6-[ [1-(N-methylcarbamoylmethyl)piperidin-4-yl]oxy]quinazoline composition and use in cancer treatment. PCT Int. Appl. (2009), 95pp. CODEN: PIXXD2 WO 2009138781 A1 20091119 CAN 151:577547 AN 2009:1433406 CAPLUS

5: Hickinson, Daniel Mark. Preparation of chlorofluoroanilinomethoxy-N- methylcarbamoylmethylpiperidinyloxyquinazoline derivatives for use as antitumor agents. PCT Int. Appl. (2010), 55pp. CODEN: PIXXD2 WO 2010061208 A2 20100603 CAN 152:592064 AN 2010:682786 CAPLUS