Cyramza ® (ramucirumab)

För fullständig produktresumé för Cyramza® se FASS.

Denna information är endast avsedd för sjukvårdspersonal verksam i Sverige och som svar på din fråga. Informationen nedan är på engelska

Cyramza® (ramucirumab): Förmåga att passera blod-hjärnbarriären

Cyramza (ramucirumab) förväntas inte passera blod-hjärnbarriären.



Detailed Information

Although not fully understood, the ability for a biologic to cross the BBB involves both specific and nonspecific interactions of biologics and receptors found on the endothelial cells of the brain capillaries. The BBB has a narrow junction, and it is believed that only molecules with a molecular weight <600 Da are able to pass through.1 It has been reported that concentration of monoclonal antibody in CSF is generally around 1000 fold lower than that in serum.2,3

The volume of distribution of ramucirumab at steady state is 5.4 liters in humans, indicating it is primarily distributed in extracellular space. Ramucirumab has a molecular weight of 146.8 kDa. Although there are no specific data on ramucirumab and its ability to cross the BBB, given the low volume of distribution and its large molecular weight, penetration of ramucirumab across the BBB is expected to be poor.4

References

1. Shi S. Biologics: an update and challenge of their pharmacokinetics. Curr Drug Metab. 2014;15(3):271-290. http://www.ingentaconnect.com/content/ben/cdm/2014/00000015/00000003/art00003

2. Tabrizi M, Bornstein GG, Suria H. Biodistribution mechanisms of therapeutic monoclonal antibodies in health and disease. AAPS J. 2010;12(1):33-43. http://dx.doi.org/10.1208/s12248-009-9157-5.

3. Curtin F, Vidal V, Bernard C, et al. Serum pharmacokinetics and cerebrospinal fluid concentration analysis of the new IgG4 monoclonal antibody GNbAC1 to treat multiple sclerosis: a phase I study. MAbs. 2016;8(5):854-860. http://dx.doi.org/10.1080/19420862.2016.1168956.

4. Data on file, Eli Lilly and Company and/or one of its subsidiaries.

Glossary

BBB = blood-brain barrier

CSF = cerebral spinal fluid

Datum fӧr senaste ӧversyn 2019 M01 11


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