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A Study to Assess the Effect of Capivasertib on Midazolam in Patients With Advanced Solid Tumours

Phase 1
Completed
Conditions
Solid Tumour
Interventions
Registration Number
NCT04958226
Lead Sponsor
AstraZeneca
Brief Summary

This is an open-label, fixed-sequence study to evaluate the effect of capivasertib on the pharmacokinetics (PK) of midazolam, a sensitive CYP3A substrate. The PK of midazolam will be assessed when administered alone and in combination with repeated doses of capivasertib.

Detailed Description

This is 2 part study: Part A and Part B. Part A of the study consists of a screening period and 3 treatment periods (midazolam alone, capivasertib alone, and midazolam + capivasertib). During Part A, the PK profile of midazolam will be determined with and without capivasertib.All participants will receive capivasertib treatment (4 days on/3 days off); however, at the Investigator's discretion, ER positive breast cancer patients may also receive fulvestrant in addition to capivasertib and midazolam. Participants completing Part A without disease progression or unacceptable toxicity, who are considered likely to continue to benefit from further capivasertib treatment (with or without certain standard of care treatment) in the opinion of the Investigator will enter Part B. Part B of the study consists of an extended treatment period with capivasertib, with or without certain standard of care treatment, followed by a 30-day safety follow-up.

Part A of the study may be extended to allow the administration of midazolam on a rescheduled Cycle 1 Day 8(C1D8) and Cycle 1 Day 12(C1D12 ) visit.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
21
Inclusion Criteria
  1. Participants with documented evidence of locally advanced inoperable or metastatic solid tumours who may be suitable to receive capivasertib treatment.
  2. Eastern Cooperative Oncology Group/World Health Organization performance status 0 to 1 and with minimum life expectancy for 12 weeks.
  3. Participant should have at least one lesion that can be assessed by computed tomography/magnetic resonance imaging or plain X-ray at baseline.
  4. Body mass index within the range 18 to 32 kg/m^2
Exclusion Criteria

Participants are excluded from the study if any of the following criteria apply:

  1. Radiotherapy with a wide field of radiation within 4 weeks of the first dose of capivasertib and/or radiotherapy with a limited field of radiation for palliation within 2 weeks prior to study intervention initiation.
  2. Participants with diabetes mellitus type I or participants with diabetes mellitus type II requiring insulin treatment.
  3. Undergone a major surgery within 4 weeks of the first dose of capivasertib.
  4. Any unresolved toxicities from prior therapies higher than CTCAE grade 2 or any unresolved toxicity that may interfere with PK assessment at the time of study intervention initiation.
  5. Participants with spinal cord compression or brain metastases.
  6. Participants with severe or uncontrolled systemic diseases, active bleeding diatheses, or active infection.
  7. Previous allogeneic bone marrow transplant or solid organ transplant.
  8. Known immunodeficiency syndrome.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SEQUENTIAL
Arm && Interventions
GroupInterventionDescription
Treatment (Midazolam + Capivasertib)MidazolamMidazolam will be administered on Cycle 1 Day 1 and Cycle 1 Day 8. Capivasertib will be administrated from Cycle 1 Day 2 as an intermittent schedule (4 days on/3 days off) until discontinuation. On Cycle 1 Day 12, Midazolam will be administrated with Capivasertib.
Treatment (Midazolam + Capivasertib)CapivasertibMidazolam will be administered on Cycle 1 Day 1 and Cycle 1 Day 8. Capivasertib will be administrated from Cycle 1 Day 2 as an intermittent schedule (4 days on/3 days off) until discontinuation. On Cycle 1 Day 12, Midazolam will be administrated with Capivasertib.
Primary Outcome Measures
NameTimeMethod
Midazolam AUCinfCycle 1 Day 1, Cycle 1 Day 2, Cycle 1 Day 8, Cycle 1 Day 9, Cycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Area under the plasma concentration-time curve from zero to infinity

Midazolam CmaxCycle 1 Day 1, Cycle 1 Day 2, Cycle 1 Day 8, Cycle 1 Day 9, Cycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Maximum observed plasma (peak) drug concentration

Secondary Outcome Measures
NameTimeMethod
Midazolam AUClastCycle 1 Day 1, Cycle 1 Day 2, Cycle 1 Day 8, Cycle 1 Day 9, Cycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Area under plasma concentration-time curve from zero to the last quantifiable concentration

Capivasertib CtroughCycle 1 Day 9 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Observed lowest drug concentration reached before the next dose is administered

Capivasertib AUCτCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Area under plasma concentration-time curve in the dose interval

Capivasertib t½λzCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Half-life associated with terminal slope (λz) of a semilogarithmic concentration-time curve

Capivasertib tmaxCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Time to reach peak or maximum observed concentration

Capivasertib CL/FCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Apparent total body clearance of drug from plasma after extravascular administration

Capivasertib metabolite AZ14102143 CtroughCycle 1 Day 9 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Observed lowest drug concentration reached before the next dose is administered

Capivasertib metabolite AZ14102143 CmaxCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Maximum observed plasma (peak) drug concentration

Capivasertib metabolite AZ14102143 AUCτCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Area under plasma concentration-time curve in the dose interval

Capivasertib metabolite AZ14102143 t½λzCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Half-life associated with terminal slope (λz) of a semilogarithmic concentration-time curve

Capivasertib metabolite AZ14102143 tmaxCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Time to reach peak or maximum observed concentration

Number of participants with adverse events and serious adverse eventsFrom screening to disease progression or discontinuation from the study (up to 15 months)

Assessment of safety and tolerability of capivasertib (with or without the use of standard of care)and in combination with midazolam.

Midazolam t½λzCycle 1 Day 1, Cycle 1 Day 2, Cycle 1 Day 8, Cycle 1 Day 9, Cycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Half-life associated with terminal slope (λz) of a semilogarithmic concentration-time curve

Midazolam tmaxCycle 1 Day 1, Cycle 1 Day 2, Cycle 1 Day 8, Cycle 1 Day 9, Cycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Time to reach peak or maximum observed concentration

Capivasertib CmaxCycle 1 Day 12 and Cycle 1 Day 13 (Cycle 1 is 29 days)

Maximum observed plasma (peak) drug concentration

Trial Locations

Locations (1)

Research Site

🇺🇸

Dallas, Texas, United States

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