A Taxane With a Unique Chemical Structure1
The role of Glycoprotein P (P-gp)
- P-gp is embedded in the membrane of normal cells in the gut, intestine, kidney, and brain, and transports potentially harmful agents out of the cell.2,3
- Transport substrates include cholesterol, peptides, proteins, toxins, antibiotics, and anticancer drugs.3
- P-gp overexpressión represents a mechanism of resistance to chemotherapy.2
JEVTANA is a Microtubular Inhibitor1
- JEVTANA binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly.1
- This leads to stabilization of microtubules and results in inhibition of mitotic and interphase cellular functions.1
The Structure of JEVTANA Demonstrates Its Pharmacodynamic Properties at the Cellular Level1
- In vitro, JEVTANA is a substrate of P-gp (P-glycoprotein), but with a low affinity. JEVTANA is not a substrate of:
- Efflux pumps MRP1 (multidrug-resistance protein 1), MRP2 (multidrug-resistance protein 2), BCRP (breast cancer resistance protein).
- SLC transporters OCT1 (organic cation transporter), OATP1B1 or OATP1B3 (organic anion transporting polypeptides).
1. JEVTANA Prescribing Information. Bridgewater, NJ: sanofi-aventis U.S. LLC; January 2018
2. Raub TJ, Mol. Pharm, 2005; 3;3-25
3. Aller SG et al., Science, 2009;323:1718-1722.
4. Sauna ZE et al, J Bioeng Biomebr. 2001; 33: 481-491