Recent Updates
Recently added Catalysts

Olaparib dosing

Phase 1

Solid Tumours | Small molecule | Oncology |AstraZeneca PLC|Last Updated: Sep 13, 2019

Success Probability

Subscribe to view

Market & Valuation

Subscribe to view

Trial Design

CONTROLLED
Total Trials3
Total Enrollment172

FDA Designations

No designations recorded

Clinical trial landscape

Olaparib dosing · 3 trials · 1 indication

Phase 1 3
NCT01894243Study to Assess the Blood Levels and Safety of Olaparib in Patients With Advanced Solid Tumours and Normal Liver Function or Mild or Moderate Liver ImpairmentSolid Tumours
COMPLETED31 Analytics
NCT01894256Study to Assess the Blood Levels and Safety of Olaparib in Patients With Advanced Solid Tumours and Normal or Impaired Kidney FunctionSolid Tumours
COMPLETED56 Analytics
NCT01900028To Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of Olaparib, and the Effect of Olaparib on QT Interval Following Oral Dosing of a Tablet Formulation to Patients With Advanced Solid TumoursSolid Tumours
COMPLETED85 Analytics
PHASE1COMPLETED
Study to Assess the Blood Levels and Safety of Olaparib in Patients With Advanced Solid Tumours and Normal Liver Function or Mild or Moderate Liver Impairment
Solid TumoursUnlock trial analytics
PHASE1COMPLETED
Study to Assess the Blood Levels and Safety of Olaparib in Patients With Advanced Solid Tumours and Normal or Impaired Kidney Function
Solid TumoursUnlock trial analytics
PHASE1COMPLETED
To Assess the Effect of Itraconazole (a CYP3A4 Inhibitor) on the Pharmacokinetics of Olaparib, and the Effect of Olaparib on QT Interval Following Oral Dosing of a Tablet Formulation to Patients With Advanced Solid Tumours
Solid TumoursUnlock trial analytics

Study Endpoints

Primary Endpoints

Maximum Plasma Concentration (Cmax)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Geometric Least Squares (GLS) Mean for normal, mild and moderate hepatic impairment

Ratio of Maximum Plasma Concentration (Cmax) - Mild vs Normal and Moderate vs Normal
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of ratio of Geometric Least Squares (GLS) Means

Area Under the Plasma Concentration Time Curve From Zero to Infinity (AUC)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Geometric Least Squares (GLS) Mean

Ratio of Area Under the Plasma Concentration Time Curve From Zero to Infinity (AUC) - Mild vs Normal and Moderate vs Normal
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Ratio of Geometric Least Squares (GLS) Means

Area Under the Plasma Concentration Time Curve From Zero to the Last Measureable Time Point(AUC 0-t)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Geometric Least Squares (GLS) Mean for ratio of mild hepatic impairment compared to normal

Ratio of Area Under the Plasma Concentration Time Curve From Zero to the Last Measureable Time Point(AUC 0-t)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Ratio of Geometric Least Squares (GLS) Means

Apparent Clearance Following Oral Administration (CL/F)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Geometric Least Squares (GLS) Means

Ratio of Apparent Clearance Following Oral Administration (CL/F)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.

Summary of Ratio of Geometric Least Squares (GLS) Means

Time to Reach Maximum Plasma Concentration (Tmax)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.
Terminal Half-life (t½)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.
Apparent Volume of Distribution (Vz/F)
Blood samples are collected at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post olaparib dose in Part A.
Cmax of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Maximum plasma drug concentration of olaparib

AUC of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Area under plasma concentration-time curve from zero to infinity of olaparib

AUC0-t of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Area under plasma concentration-time curve from zero to the last measurable time point of olaparib

Tmax of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Time to reach maximum plasma concentration of olaparib

Vz/F of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Apparent volume of distribution of olaparib

CL/F of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Apparent plasma clearance of olaparib

CLR of Olaparib
Part A: Day 1, 0-12 hours and 12-24 hours post-dose

Renal clearance of olaparib, calculated as the ratio of amount of drug excreted over 24 hours to AUC0-24

t1/2 of Olaparib
Part A: pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, 72 and 96 hours post-dose

Terminal half-life of olaparib

Pharmacokinetics of olaparib by assessment of maximum plasma olaparib concentration (Cmax)
Blood samples are collected on Day 1& Day 9 at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A. Part B:Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose

Rate and extent of absorption of olaparib following single (Part A) and multiple (Part B) oral doses of olaparib tablet formulation by assessment of maximum plasma olaparib concentration (Cmax)

Pharmacokinetics of olaparib by assessment of area under the plasma concentration time curve from zero to infinity (AUC)
Blood samples are collected on Day 1& Day 9 at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A. Part B:Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose

Rate and extent of absorption of olaparib following single (Part A) and multiple (Part B) oral doses of olaparib tablet formulation by assessment of area under the plasma concentration time curve from zero to infinity (AUC)

Pharmacokinetics of olaparib by assessment of area under the plasma concentration time curve from zero to the last measurable time point, AUC0-t, if AUC is not adequately estimable).
Blood samples are collected on Day 1& Day 9 at pre-dose, 0.25 , 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, and 72 hours post olaparib dose Part A. Part B:Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose

Rate and extent of absorption of olaparib following single (Part A) and multiple (Part B) oral doses of olaparib tablet formulation by assessment of area under the plasma concentration time curve from zero to the last measurable time point, (AUC0-t)

Secondary Endpoints

Pharmacokinetics of olaparib by assessment of time to reach maximum plasma concentration for olaparib (tmax)
PK samples taken on Day 1 & Day 9 at pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, & 72 hours post dose (Part A). And in Part B, Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose
Pharmacokinetics of olaparib by assessment of area under the plasma concentration time curve from zero to the last measurable time point (AUC0-τ)
PK samples taken on Day 1 & Day 9 at pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, & 72 hours post dose (Part A). And in Part B, Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose
Pharmacokinetics of olaparib by assessment of time olaparib apparent clearance (CL/F)
PK samples taken on Day 1 & Day 9 at pre-dose, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24, 48, & 72 hours post dose (Part A). And in Part B, Day 5 at pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post dose
Unlock Study Endpoints

Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeOTHER

Treatment Arms

ArmTypeDescription
Normal hepatic functionOTHERPatients with: (i) negative result for serum hepatitis B surface antigen and hepatitis C antibody (ii) total bilirubin ≤1.5 x institutional upper limit of normal (ULN), albumin and prothrombin time within normal limits and must not have ascites (unless related to disease under study) or encephalopathy (iii) aspartate aminotransferase or serum glutamic oxaloacetic transaminase (AST), alanine aminotransferase or serum glutamic pyruvic transaminase (ALT) ≤2.5 x institutional ULN unless liver metastases are present in which case it must be ≤5 x ULN
Mild hepatic impairmentOTHERAs defined by the Child-Pugh Classification System.
Moderate hepatic impairmentOTHERAs defined by the Child-Pugh Classification System.
Normal renal functionOTHERPatients with calculated serum creatinine clearance ≥81 mL/min (using Cockcroft-Gault equation).
Mild renal impairmentOTHERPatients with calculated serum creatinine clearance 51-80 mL/min (using Cockcroft-Gault equation).
Moderate renal impairmentOTHERPatients with calculated serum creatinine clearance 31-50 mL/min (using Cockcroft-Gault equation).
Olaparib alone, olaparib+itraconozoleEXPERIMENTALSequential treatments of olaparib alone followed by olaparib+itraconazole, with a washout period in between.

Interventions

NameTypeDescription
Olaparib tablet dosingDRUGPart A - single 300mg oral dose olaparib (administered as 2x150mg tablets) Part B - 300mg oral dose olaparib (administered as 2x150mg tablets) bd
Pharmacokinetic samplingPROCEDUREBlood samples taken pre and post dosing with olaparib+/- itraconazole
ItraconazoleDRUGItraconazole 200mg od Part A days 5 to 11 only
Unlock Study Design Details

Eligibility Criteria

Age Range18 Years to 130 Years
SexALL
Healthy VolunteersNo
Study Sites12

Inclusion criteria:- For inclusion in the study as a patient with hepatic impairment, the following criterion must be met: 1. Patients must have stable mild hepatic impairment (as defined by Child-Pugh classification), for at least 1 month prior to the start of the study or stable moderate hepatic...

Countries:CzechiaFranceNetherlandsSouth KoreaUnited KingdomBelgiumDenmark
Unlock Eligibility Criteria

Competitive Landscape -Other Solid Tumors 9 trials (matched to "Solid Tumours")

Frequently asked questions about Olaparib dosing

What is olaparib used for?

Olaparib is an investigational small molecule being studied for the treatment of advanced solid tumours. It is currently in Phase 1 clinical development, with studies assessing its blood levels, safety, and effects on the QT interval in patients with advanced solid tumours.

Who makes olaparib?

Olaparib is being developed by AstraZeneca PLC, a biopharmaceutical company listed on the stock exchange under the ticker symbol AZN. The company is conducting Phase 1 clinical trials to evaluate the drug in patients with advanced solid tumours.

What phase is olaparib in?

Olaparib is in Phase 1 clinical development. It is an investigational drug, meaning it has not yet been approved by regulatory authorities. All three completed trials involving olaparib are Phase 1 studies focused on assessing its pharmacokinetics and safety in patients with advanced solid tumours.

What clinical trials is olaparib in?

Olaparib has been studied in three completed Phase 1 clinical trials: NCT01894243, NCT01894256, and NCT01900028. These trials assessed blood levels and safety in patients with advanced solid tumours and normal or impaired liver or kidney function, as well as the effect of itraconazole on olaparib pharmacokinetics and QT interval.

How does olaparib work?

Olaparib is a small molecule being studied for its effects in advanced solid tumours. The specific molecular target of olaparib has not been disclosed in the available clinical trial information, so its mechanism of action is not described here.

Is olaparib the same as any other drug?

Olaparib is the drug name used in the clinical trials, and no alternative names have been reported. It is being developed by AstraZeneca PLC under this name for the treatment of advanced solid tumours.