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Idasanutlin

Phase 1

Solid Tumors | Small molecule | Oncology |Roche Holding AG|Last Updated: Jun 19, 2019

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials2
Total Enrollment56

FDA Designations

No designations recorded

Clinical trial landscape

Idasanutlin · 2 trials · 1 indication

Phase 1 2
NCT03362723A Study to Investigate the Bioequivalence or Relative Bioavailability of Three New Idasanutlin Tablet Variants Following Oral Administration in Participants With Solid TumorsSolid Tumors
COMPLETED48 Analytics
NCT02828930A Study to Determine the Excretion Balance, Pharmacokinetics, Metabolism and Absolute Oral Bioavailability of a Single Oral Dose of [14C]-Labeled Idasanutlin and an Intravenous Tracer Dose of [13C]-Labeled Idasanutlin in a Single Cohort of Participants With Solid Tumors (Malignancies)Solid Tumors
COMPLETED8 Analytics
PHASE1COMPLETED
A Study to Investigate the Bioequivalence or Relative Bioavailability of Three New Idasanutlin Tablet Variants Following Oral Administration in Participants With Solid Tumors
Solid TumorsUnlock trial analytics
PHASE1COMPLETED
A Study to Determine the Excretion Balance, Pharmacokinetics, Metabolism and Absolute Oral Bioavailability of a Single Oral Dose of [14C]-Labeled Idasanutlin and an Intravenous Tracer Dose of [13C]-Labeled Idasanutlin in a Single Cohort of Participants With Solid Tumors (Malignancies)
Solid TumorsUnlock trial analytics

Study Endpoints

Primary Endpoints

Area Under the Curve (AUC) of Idasanutlin
Predose (within 2 hours), 1, 2, 4, 6, and 10 hours on Days 1, 8, 15, and 22; on Days 2, 3, 5, 9, 10, 12, 16, 17, 19, 23, 24, and 26; Day 29 (end of Cycle 1) or Cycle 2 Day 1 (for participants in the optional treatment extension phase) (cycle=28 days)
Maximum Observed Plasma Concentration (Cmax) of Idasanutlin
Predose (within 2 hours), 1, 2, 4, 6, and 10 hours on Days 1, 8, 15, and 22; on Days 2, 3, 5, 9, 10, 12, 16, 17, 19, 23, 24, and 26; Day 29 (end of Cycle 1) or Cycle 2 Day 1 (for participants in the optional treatment extension phase) (cycle=28 days)
Time to Reach Maximum Observed Plasma Concentration (Tmax) of Unlabeled Idasanutlin
0 Hour (hr) predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Maximum Observed Plasma Concentration (Cmax) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Area Under the Plasma Concentration Time-Curve From Time Zero to Extrapolated Infinite Time (AUC [0-inf]) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Area Under the Plasma Concentration Time-Curve From Zero to the Last Measured Concentration (AUC[0-last]) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Plasma Elimination Half-Life (t1/2) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Plasma Apparent Elimination Rate Constant of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Apparent Oral Clearance (CL/F) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Renal Clearance (CLr) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Apparent Volume of Distribution (Vz/F) of Unlabeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Cumulative Amount Excreted in Urine of Unlabeled Idasanutlin
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
Cumulative Amount Excreted in Feces of Unlabeled Idasanutlin
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
Tmax of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Cmax of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
AUC (0-inf) of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
AUC(0-last) of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Plasma t1/2 of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Plasma Apparent Elimination Rate Constant of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
CL/F of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
CLr of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Vz/F of Idasanutlin Metabolite
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Cumulative Amount Excreted in Urine of Idasanutlin Metabolite
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
Cumulative Amount Excreted in Feces of Idasanutlin Metabolite
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
Tmax of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55 minutes (min), 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Cmax of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55 min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
AUC(0-inf) of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55 min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
AUC(0-last) of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Plasma t1/2 of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Absolute Oral Bioavailability of [13C]-Labeled Idasanutlin
Oral administration: 0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose; IV administration: 0 hr predose, 5hr 55min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Whole Blood and Plasma Cmax of [14C]-Labeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Whole Blood and Plasma AUC(0-inf) of [14C]-Labeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Whole Blood and Plasma AUC(0-last) of [14C]-Labeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Whole Blood and Plasma Apparent Elimination Rate Constant of [14C]-Labeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Cumulative Amount of Radioactivity Excreted in Urine as Percentage of Dosed Radioactivity of [14C]-Labeled Idasanutlin
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
Cumulative Amount of Radioactivity Excreted in Feces as Percentage of Dosed Radioactivity of [14C]-Labeled Idasanutlin
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose
CL/F of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Vz/F of [13C]-Labeled Idasanutlin
0 hr predose, 5hr 55min, 6hr, 6hr 5min, 6hr 10min, 6hr 15min, 6hr 30min, 7, 10, 24, 48, 96, 120, 144, 240 hrs postdose
Whole Blood and Plasma Tmax of [14C]-Labeled Idasanutlin
0 hr predose, 1, 3, 6, 7, 24, 48, 96, 120, 144, 240 hrs postdose
Cumulative Amount of Radioactivity Excreted in Feces on Toilet Tissue as Percentage of Dosed Radioactivity of [14C]-Labeled Idasanutlin
0 hr (within 24 hrs of dosing), pooled sample collected over time interval: 0-6, 6-12, 12-24, 24-48, 48-72, 72-96, 96-120, 120-144, 144-168, 168-192, 192-216, 216-240, 240-264 hrs postdose

Secondary Endpoints

Time to Maximum Observed Plasma Concentration (tmax) of Idasanutlin
Predose (within 2 hours), 1, 2, 4, 6, and 10 hours on Days 1, 8, 15, and 22; on Days 2, 3, 5, 9, 10, 12, 16, 17, 19, 23, 24, and 26; Day 29 (end of Cycle 1) or Cycle 2 Day 1 (for participants in the optional treatment extension phase) (cycle=28 days)
Apparent Clearance (CL/F) of Idasanutlin
Predose (within 2 hours), 1, 2, 4, 6, and 10 hours on Days 1, 8, 15, and 22; on Days 2, 3, 5, 9, 10, 12, 16, 17, 19, 23, 24, and 26; Day 29 (end of Cycle 1) or Cycle 2 Day 1 (for participants in the optional treatment extension phase) (cycle=28 days)
Apparent Volume of Distribution (Vd/F) of Idasanutlin
Predose (within 2 hours), 1, 2, 4, 6, and 10 hours on Days 1, 8, 15, and 22; on Days 2, 3, 5, 9, 10, 12, 16, 17, 19, 23, 24, and 26; Day 29 (end of Cycle 1) or Cycle 2 Day 1 (for participants in the optional treatment extension phase) (cycle=28 days)
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Treatment Sequence 1: ABCDEXPERIMENTALTreatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 1 (one cycle is 28 days). Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 8. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 15. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description.
Treatment Sequence 2: ABDCEXPERIMENTALTreatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 1 (one cycle is 28 days). Treatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 8. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 15. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description.
Treatment Sequence 3: BACDEXPERIMENTALTreatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 1 (one cycle is 28 days). Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 8. Treatment C: A single dose of new idasanutlin tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 15. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description.
Treatment Sequence 4: BADCEXPERIMENTALTreatment B: A single dose of new idasanutlin tablet B (to investigate BE compared to tablet A) on Cycle 1, Day 1 (one cycle is 28 days). Treatment A: A single dose of the current idasanutlin tablet A formulation (reference variant) on Cycle 1, Day 8. Treatment D: A single dose of new idasanutlin tablet D (to investigate rBA compared to tablet A; rBA 2) on Cycle 1, Day 15. Treatment C: A single dose of new tablet C (to investigate rBA compared to tablet A; rBA 1) on Cycle 1, Day 22. Following completion of the BE/rBA cycle (Cycle 1), participants may continue to receive optional treatment cycles of the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description.
Optional Treatment Extension ArmEXPERIMENTALFollowing completion of the BE/rBA cycle (Cycle 1), participants who have no clinically defined progressive disease per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1) and who recover from any prior treatment toxicity to Grade \</=1 may enter the optional treatment extension phase. Participants will receive 200 mg idasanutlin orally (200-mg tablet reference formulation) daily for 5 days, followed by 23 days of rest. This extension phase will continue for additional 28-day cycles or until disease progression or unacceptable toxicity is observed.
IdasanutlinEXPERIMENTALOn Day 1, 300 milligram (mg) idasanutlin tablet orally and 100 mg \[14C\]-radiolabeled idasanutlin capsule orally (2, 50 mg capsules containing approximately 100 microcurie of radioactivity). After 5 hours and 45 minutes of the oral dose, 100 microgram (mcg) of \[13C\]-radiolabeled idasanutlin will be administered over a 15-minute intravenous (IV) infusion. On Day 11, idasanutlin matching placebo aqueous dispersion orally and approximately after 1 hour, 400 mg idasanutlin tablet will be administered orally in the form of an aqueous dispersion. On Day 19, 400 mg idasanutlin tablet will be administered orally in the form of an aqueous dispersion. Participants, who are eligible to enter in optional treatment extension phase, will continue treatment with idasanutlin 200 mg tablet orally once daily for 5 days, and no treatment during 23 days of 28-day cycle, until the development of progressive disease, unacceptable toxicity, consent withdrawal or any other criteria for removal.

Interventions

NameTypeDescription
IdasanutlinDRUGParticipants will receive one 300-mg dose of each of the four different oral tablet formulations of idasanutlin (tablet A \[reference\], B, C, D) during Cycle 1, in the order specified for their assigned treatment arm (Treatment Sequence 1-4). Participants who enter the optional treatment extension phase will receive the reference tablet formulation of idasanutlin, as specified in the Optional Treatment Extension Arm description.
PlaceboDRUGPlacebo matching to idasanutlin aqueous dispersion will be administered orally on Day 11.
[13C]-radiolabeled IdasanutlinDRUG\[13C\]-radiolabeled idasanutlin 100 mcg will be administered as IV infusion over 15-minute on Day 1.
[14C]-radiolabeled IdasanutlinDRUG\[14C\]-radiolabeled idasanutlin 100 mg capsule (2, 50 mg capsules containing approximately 100 microcurie of radioactivity) will be administered orally on Day 1.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites11

Inclusion Criteria: * Participant must have histologically or cytologically confirmed advanced malignancies, except all forms of leukemia and lymphoma, for which standard curative or palliative measures do not exist, are no longer effective, or are not acceptable to the participant * Measureable or...

Countries:United StatesCanadaHungary
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Competitive Landscape -Other Solid Tumors 9 trials (matched to "Solid Tumors")

Frequently asked questions about Idasanutlin

What is Idasanutlin used for in solid tumors?

Idasanutlin is an investigational small molecule being studied for the treatment of solid tumors. It is currently in Phase 1 clinical development. The drug is being evaluated in adult patients with solid tumors, including malignancies, to assess its pharmacokinetics, metabolism, and bioavailability.

Who makes Idasanutlin?

Idasanutlin is being developed by Roche Holding AG, a pharmaceutical company traded under the ticker RHHBY. Roche is conducting clinical trials to evaluate the drug's properties in patients with solid tumors.

What phase is Idasanutlin in?

Idasanutlin is in Phase 1 clinical development. It is an investigational drug and has not been approved by regulatory authorities. Two Phase 1 trials have been completed, both involving patients with solid tumors.

What clinical trials is Idasanutlin in?

Idasanutlin has been studied in two completed Phase 1 trials. NCT02828930 examined the excretion balance, pharmacokinetics, metabolism, and absolute oral bioavailability of a single oral dose of radiolabeled Idasanutlin in 8 participants with solid tumors in Hungary. NCT03362723 investigated the bioequivalence of three new tablet variants in 48 participants in the United States and Canada.

Is Idasanutlin the same as any other drug?

Idasanutlin is a distinct investigational small molecule developed by Roche. No alternative names for this drug have been reported in the clinical trial records. It is being studied specifically for its properties in patients with solid tumors.