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Approved anticancer agents

Anticancer agents in trials

Anticancer molecular libraries

MedKoo product information:

 Verubulin

MPC-6827 is a quinazoline derivative with potential dual antineoplastic activities. MPC-6827 binds to and inhibits tubulin polymerization and interrupts microtubule formation, resulting in disruption of mitotic spindle assembly, cell cycle arrest in the G2/M phase, and cell death. This agent is not a substrate for several subtypes of multidrug resistance ABC transporters, such as P-glycoprotein, multidrug resistance-associated protein 1 (MRP1), and breast cancer resistance protein 1 (BCRP1); therefore, it may be useful for treating multidrug resistant (MDR) tumors that express these transporters. In addition, as a vascular disrupting agent (VDA), MPC-6827 appears to disrupt tumor microvasculature specifically, which may result in acute ischemia and massive tumor cell death.

According to Myriad's website, Azixa is a novel, small-molecule that acts as a microtubule destabilizing agent, causing arrest of cell division and programmed cell death, or apoptosis, in cancer cells. Azixa has also been shown to be a vascular disrupting agent (VDA) in a mouse model of human ovarian cancer. Thus, Azixa has a dual mode of action; it induces apoptosis and reduces blood supply to the tumor. Importantly, in non-clinical studies, Azixa has demonstrated the unique ability to effectively cross the blood-brain barrier and accumulate in the brain at levels as much as 30-fold that in plasma and does not appear to be subject to multiple drug resistance.  Azixa is currently being tested in clinical studies in patients with glioblastoma multiforme and metastatic melanoma. see: http://www.myriadpharma.com/product-pipeline/clinical/azixa.

 Current developer:   Myriad Pharmaceuticals.

1. Foucourt, Alicia; Dubouilh-Benard, Carole; Chosson, Elizabeth; Corbiere, Cecile; Buquet, Catherine; Iannelli, Mauro; Leblond, Bertrand; Marsais, Francis; Besson, Thierry. Microwave-accelerated Dimroth rearrangement for the synthesis of 4-anilino-6-nitroquinazolines. Application to an efficient synthesis of a microtubule destabilizing agent. Tetrahedron (2010), 66(25), 4495-4502.

2. Sirisoma, Nilantha; Pervin, Azra; Zhang, Hong; Jiang, Songchun; Adam Willardsen, J.; Anderson, Mark B.; Mather, Gary; Pleiman, Christopher M.; Kasibhatla, Shailaja; Tseng, Ben; Drewe, John; Cai, Sui Xiong. Discovery of N-methyl-4-(4-methoxyanilino)quinazolines as potent apoptosis inducers. Structure-activity relationship of the quinazoline ring. Bioorganic & Medicinal Chemistry Letters (2010), 20(7), 2330-2334. 

3. Hanrahan, Emer O.; Kies, Merrill S.; Glisson, Bonnie S.; Khuri, Fadlo R.; Feng, Lei; Tran, Hai T.; Ginsberg, Lawrence E.; Truong, Mylene T.; Hong, Waun K.; Kim, Edward S. A phase II study on lonafarnib (SCH66336) in patients with chemorefractory, advanced squamous cell carcinoma of the head and neck. American Journal of Clinical Oncology (2009), 32(3), 274-279. 

4. Sirisoma, Nilantha; Pervin, Azra; Zhang, Hong; Jiang, Songchun; Willardsen, J. Adam; Anderson, Mark B.; Mather, Gary; Pleiman, Christopher M.; Kasibhatla, Shailaja; Tseng, Ben; Drewe, John; Cai, Sui Xiong. Discovery of N-(4-Methoxyphenyl)-N,2-dimethylquinazolin-4-amine, a Potent Apoptosis Inducer and Efficacious Anticancer Agent with High Blood Brain Barrier Penetration. Journal of Medicinal Chemistry (2009), 52(8), 2341-2351. 

5. Kasibhatla, Shailaja; Baichwal, Vijay; Cai, Sui Xiong; Roth, Bruce; Skvortsova, Ira; Skvortsov, Sergej; Lukas, Peter; English, Nicole M.; Sirisoma, Nilantha; Drewe, John; Pervin, Azra; Tseng, Ben; Carlson, Robert O.; Pleiman, Christopher M. MPC-6827: A small-molecule inhibitor of microtubule formation that is not a substrate for multidrug resistance pumps. Cancer Research (2007), 67(12), 5865-5871.