Back to products

Browse products

Approved anticancer agents

Anticancer agents in trials

Anticancer molecular libraries

Other drug agents

Bio-reagents and biochemicals

MedKoo product information:

Description of Rosabulin: rosabulin (STA-5312) is a novel microtubule inhibitor with a distinct binding site from other agents such as vincristine, colchicine, or paclitaxel, which has demonstrated antitumor activity against a range of solid tumors in chemotherapy-resistant cancer. Phase I study showed that STA-5312 appears to be well tolerated when given weekly in doses up to 32mg/m2. The MTD has not been determined and enrollment is ongoing. (source: asco.org)

Current developer:  Synta Pharmaceuticals Corp.

STA-5312, 2-[3-(4-cyano-benzyl)-indolizin-1-yl]-N-(3-methyl-isothiazol-5-yl)-2-oxo-acetamide, is a new chemical entity being developed for the treatment of chemotherapy-resistant tumors. STA-5312 demonstrates substantial anti-proliferative activity against a wide range of cancer cell linesin vitro, with IC₅₀ values extending down into the nanomolar range. The in vitro cytotoxic effects have been demonstrated across a wide array of tumor types, including hematologic and solid tumor cell lines of various origins (e.g. leukemia, lymphoma, breast, colon, uterine). Cell lines with multi-drug resistant (MDR) phenotypes were similarly sensitive to STA-5312. The mechanism of action for STA-5312 is inhibition of microtubule assembly and subsequent arrest of the cell cycle. STA-5312 is active against several tumor cell lines that express moderate to high levels of P-glycoprotein (Pgp), including lines insensitive to Taxol, Vincristine, and Adriamycin in which Pgp activity is a major contributor to the MDR phenotype. When dosed orally or intravenously, STA-5312 has shown in vivo activity in several murine tumors as well as human tumor xenograft models, including drug resistant tumors. Data on the murine leukemia P388 suggested activity in a vincristine-resistant cell line, and data in the RL human Lymphoma cell line suggested an additive effect of Taxol plus STA-5312. Thus, STA-5312 is a potential new therapy for the treatment of cancer including chemoresistant tumors. Considering the breadth of antitumor activity demonstrated by STA-5312 both in vitro and in vivo, two lines of clinical investigation are envisioned encompassing both hematologic and solid tumors. see: Synta Pharmaceuticals Corp's meeting abstract.

STA-5312 inhibits microtubule function, critical to cancer cell proliferation, through a unique binding site. Ongoing phase 1 studies of STA- 5312 in hematological and solid tumor malignancies are expected to be completed in the first half of 2006. The study findings will guide future clinical investment decisions for the compound.

 1: Chen G, Wang ZQ, Jia JM. Three minor novel triterpenoids from the leaves of Diospyros kaki. Chem Pharm Bull (Tokyo). 2009 May;57(5):532-5. PubMed PMID: 19420791.

2: Park JC, Kim SC, Choi MR, Song SH, Yoo EJ, Kim SH, Miyashiro H, Hattori M. Anti-HIV protease activity from rosa family plant extracts and rosamultin from Rosa rugosa. J Med Food. 2005 Spring;8(1):107-9. PubMed PMID: 15857219.

3: Cheol Park J, Chul Kim S, Moon Hur J, Choi SH, Yeon Lee K, Won Choi J. Anti-hepatotoxic effects of Rosa rugosa root and its compound, rosamultin, in rats intoxicated with bromobenzene. J Med Food. 2004 Winter;7(4):436-41. PubMed PMID: 15671686.

4: Jung HJ, Nam JH, Choi J, Lee KT, Park HJ. 19Alpha-hydroxyursane-type triterpenoids: antinociceptive anti-inflammatory principles of the roots of Rosa rugosa. Biol Pharm Bull. 2005 Jan;28(1):101-4. PubMed PMID: 15635171.

5: Cho EJ, Yokozawa T, Rhyu DY, Kim HY, Shibahara N, Park JC. The inhibitory effects of 12 medicinal plants and their component compounds on lipid peroxidation. Am J Chin Med. 2003;31(6):907-17. PubMed PMID: 14992543.

6: Lu X, Xu W, Shen J, Han G. [Chemical studies on Campylotropis hirtella (Franch. Schindl.)]. Zhongguo Zhong Yao Za Zhi. 1997 Nov;22(11):680-2, 704. Chinese. PubMed PMID: 11243186.

7: Rücker G, Mayer R, Shin-Kim JS. [Triterpene saponins from the Chinese drug "Daxueteng" (Caulis sargentodoxae)]. Planta Med. 1991 Oct;57(5):468-70. German. PubMed PMID: 1798803.

8: Wang XY. [Effects of constituents of the roots of Rosa multiflora on hyperlipemia]. Zhong Yao Tong Bao. 1986 Jun;11(6):55-6. Chinese. PubMed PMID: 2948697.