MedKoo product information:

Epofolate

Description of Epofolate: Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

Current developer:    Endocyte Inc. and Bristol Myers Squibb (BMS).

Epofolate is a synthetic conjugate of Epothilone and folic acid. Epofolate is currently investigated by Bristol-Myers Squibb as an anticancer drug candidate. As of 2010, this agent is in Phase 1/2 clinical study. The purpose of this clinical research study is to study the safety of Epofolate (BMS-753493) in patients with advanced cancers (in Phase 1 portion) and to determine whether Epofolate (BMS-753493) can shrink or slow the growth of the cancer in patients with advanced ovarian, renal or breast cancer (in Phase 2 portion).  Assigned Interventions: Intravenous solution, intravenous, initially 3 patients will be treated and if there is a DLT then additional 3 patients will be treated in that dose level. 3-5 minute IV bolus on Days 1 through 4 of a 21-day cycle, until the disease progresses (source: http://clinicaltrials.gov/ct2/show/NCT00546247).

BMS-753493 is a molecule born from a collaboration between scientists at Endocyte Inc. and Bristol Myers Squibb (BMS). It represents a FA conjugate that was constructed with a semi-synthetic analog of Epothilone A. BMS-753493 is currently being evaluated for safety and efficacy in Phase 2 clinical trials sponsored by BMS. 

1: Vlahov IR, Vite GD, Kleindl PJ, Wang Y, Santhapuram HK, You F, Howard SJ, Kim  SH, Lee FF, Leamon CP. Regioselective synthesis of folate receptor-targeted agents derived from epothilone analogs and folic acid. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4578-81. Epub 2010 Jun 8. PubMed PMID: 20594844.

2: Eng C, Kindler HL, Nattam S, Ansari RH, Kasza K, Wade-Oliver K, Vokes EE. A phase II trial of the epothilone B analog, BMS-247550, in patients with previously treated advanced colorectal cancer. Ann Oncol. 2004 Jun;15(6):928-32.  PubMed PMID: 15151950.

3: Sternberg CN, Vogelzang NJ. Gemcitabine, paclitaxel, pemetrexed and other newer agents in urothelial and kidney cancers. Crit Rev Oncol Hematol. 2003 Jun 27;46 Suppl:S105-15. Review. PubMed PMID: 12850531.