title: Levels of Sirolimus in saliva vs. blood--the rationale of topical oral use for oral malignancy.
abstract: BACKGROUND
  Sirolimus is a potent blocker of mammalian target of Rapamycin (MTOR), with anti proliferative activity. Its potential for the management of oral cancer has been suggested. Our aim was to establish an analytical method for determining sirolimus levels in human saliva and to calculate the blood vs. saliva ratio in individuals using sirolimus chronically in order to evaluate the total oral tissue exposure.
  
  
  METHODS
  Chemiluminescent microparticle immunoassay technology (CMIA) was used to determine the blood and saliva levels of sirolimus in four transplant patients chronically-treated with sirolimus.
  
  
  RESULTS
  An analytical method for determining sirolimus levels in human saliva was established. We demonstrated that saliva levels were on average six times lower than blood levels.
  
  
  CONCLUSIONS
  The specific sensitive analytical method showed that the saliva levels of sirolimus are significantly lower than blood levels, thus reinforcing the rationale for the use of topical oral sirolimus to enhance availability, efficacy and safety for treating oral malignancies.
authors: Department of Oral Medicine, Hebrew University - Hadassah School of Dental Medicine, Qiryat Hadassah PO Box. 12272, Jerusalem, 91120, Israel.
authors: Zakhar
authors: Z
authors: Nudelman
authors: Naama
authors: N
authors: Keshet
authors: Michal Dranitzki
authors: MD
authors: Elhalal
authors: Michael
authors: M
authors: Friedman
authors: Rakefet
authors: R
authors: Czerninski
mesh_terms: D000287:Administration, Topical; D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000032:analysis* / Q000493:pharmacokinetics; D005260:Female; D006084:Graft Rejection / Q000517:prevention & control; D006801:Humans; D007118:Immunoassay / Q000379:methods*; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics; D016030:Kidney Transplantation; D008163:Luminescent Measurements / Q000379:methods*; D008297:Male; D008875:Middle Aged; D009062:Mouth Neoplasms / Q000188:drug therapy; D012463:Saliva / Q000737:chemistry*; D020123:Sirolimus / Q000008:administration & dosage / Q000032:analysis* / Q000493:pharmacokinetics
chemical_list: D000970:Antineoplastic Agents; D007166:Immunosuppressive Agents; D020123:Sirolimus