A randomized, open label, two-way crossover study investigating the relative bioavailability of a single 5 mg dose of everolimus administered as either 5x1 mg everolimus intact tablets or 5x1 mg everolimus tablets suspended in 30 mL of water to healthy subjects
- Conditions
- Healthy volunteersTherapeutic area: Diseases [C] - Cancer [C04]
- Registration Number
- EUCTR2012-000299-40-Outside-EU/EEA
- Lead Sponsor
- ovartis Pharma Services AG
- Brief Summary
Not available
- Detailed Description
Not available
Recruitment & Eligibility
- Status
- A
- Sex
- All
- Target Recruitment
- 40
• Female or male healthy subjects from 18 to 55 years of age;
• Female subjects must be postmenopausal (no menstrual bleeding for 12 months), or surgically sterilized at least 6 months prior to screening;
• Good health status as determined by past medical history, physical examination, vital signs, electrocardiogram and laboratory tests within normal ranges at screening;
• Vital signs (after 3 minutes resting measured in the supine position) must be within the ranges specified in the protocol
Are the trial subjects under 18? no
Number of subjects for this age range:
F.1.2 Adults (18-64 years) yes
F.1.2.1 Number of subjects for this age range 40
F.1.3 Elderly (>=65 years) no
F.1.3.1 Number of subjects for this age range
• Smokers defined as having used tobacco products in the previous 3 months or having urine cotinine levels greater than 500 ng/mL tested at screening and each baseline visit;
• Use of any prescription medication within 1 month prior to dosing or any over-the-counter (OTC) medication within 2 weeks prior to dosing;
• Consumption of grapefruit products within 1 week prior to dosing;
• Participation in any clinical investigation within 4 weeks prior to dosing;
• Donation or loss of 450 mL or more of blood within 56 days prior to dosing;
• Women who are of child-bearing potential, or pregnant, or breast feeding (positive serum pregnancy test for ß-hCG at screening and each baseline visit);
• A known hypersensitivity to rapamycins and their derivates or drugs similar to RAD001, e.g. macrolides;
• Any subject who has been diagnosed with type I or II diabetes, hyperglycemia or impaired glucose intolerance;
• History of any significant respiratory system chronic brochospastic disease (including asthma and COPD, treated or not treated).
• History of atopic allergy (asthma, urticaria, eczematous dermatitis);
• Any surgical or medical condition which might significantly alter the absorption, distribution, metabolism or excretion of drugs or which may jeopardize the subject in case of participation in the study.
• History of immunosuppression, including a known positive HIV test result;
• A positive Hepatitis B surface antigen (HBsAg) or Hepatitis C test result;
• Evidence of alcohol and drug usage as indicated by laboratory assays performed at screening and prior to baseline period.
Study & Design
- Study Type
- Interventional clinical trial of medicinal product
- Study Design
- Not specified
- Primary Outcome Measures
Name Time Method Main Objective: To evaluate the bioavailability of: <br>5 x 1 mg everolimus intact tables, and<br>5 x 1 mg everolimus tablets suspended in 30 mL of water;Secondary Objective: To evaluate the safety and tolerability of the 1 mg everolimus tablets administered as suspension and as intact tablets;Primary end point(s): Primary pharmacokinetic parameters: AUC(0-t), AUC(0-inf) and Cmax;Timepoint(s) of evaluation of this end point: Full pharmacokinetic whole blood samples will be drawn at each of the two treatment periods as follows: 1 pre-dose sample < 15min prior to administration of study drug and 17 postdose<br>samples at 0.5 h, 1 h, 1.5 h, 2 h, 2.5 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h and 144 h after administration of study drug.
- Secondary Outcome Measures
Name Time Method Secondary end point(s): - Secondary pharmacokinetic parameters: Tmax, ?z, Vd/F, CL/F and t1/2<br>- Safety endpoints (evaluation of adverse events and serious adverse events, vital signs, ECG, laboratory results (hematology, blood chemistry, urinalysis);Timepoint(s) of evaluation of this end point: - Full pharmacokinetic whole blood samples will be drawn at each of the two treatment periods as follows: 1 pre-dose sample < 15min prior to administration of study drug and 17 postdose<br>samples at 0.5 h, 1 h, 1.5 h, 2 h, 2.5 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h and 144 h after administration of study drug.<br>- Safety laboratory assessments will be performed regularly. Hematology and biochemistry laboratory parameters will be evaluated at screening, each of the 2 baseline visits, 144 hours post-dose and at the study completion visit.