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¿Cuál es el mecanismo de Acción de Jevtana?

A Taxane With a Unique Chemical Structure1

 

 

 

 

 

 

The role of Glycoprotein P (P-gp)mecanismo  acción

  • 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).

References:

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