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Enzalutamide

Phase 1

Neoplasms | Small molecule | Oncology |Roche Holding AG|Last Updated: Jan 12, 2022

Target and mechanism

Molecular targetAR
Target classAntagonist
ModalitySmall molecule

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment122

FDA Designations

No designations recorded

Clinical trial landscape

Enzalutamide · 1 trial · 1 indication

Phase 1 1
NCT01362374Safety and Clinical Pharmacology of GDC-0068 in Combination With Docetaxel, Fluoropyrimidine Plus Oxaliplatin, Paclitaxel, or Enzalutamide in Participants With Advanced Solid TumorsNeoplasms
COMPLETED122 Analytics
PHASE1COMPLETED
Safety and Clinical Pharmacology of GDC-0068 in Combination With Docetaxel, Fluoropyrimidine Plus Oxaliplatin, Paclitaxel, or Enzalutamide in Participants With Advanced Solid Tumors
NeoplasmsUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Participants With Dose Limiting Toxicities (DLTs)
Arm A: Days 2-21 of Cycle 1 (cycle length=21 days); Arm B: Days 1-14 of Cycles 1 and 2 (cycle length=14 days); Arm C: Days 1-28 of Cycle 1 (cycle length=28 days); Arm D: Days 1-35 of Cycle 1 (cycle length=28 days except for Cycle 1=35 days)
Maximum Tolerated Dose (MTD) of Ipatasertib
Arm A: Days 2-21 of Cycle 1 (cycle length=21 days); Arm B: Days 1-14 of Cycles 1 and 2 (cycle length=14 days); Arm C: Days 1-28 of Cycle 1 (cycle length=28 days); Arm D: Days 1-35 of Cycle 1 (cycle length=28 days except for Cycle 1=35 days)
Recommended Phase II Dose (RP2D) of Ipatasertib
Arm A: Days 2-21 of Cycle 1 (cycle length=21 days); Arm B: Days 1-14 of Cycles 1 and 2 (cycle length=14 days); Arm C: Days 1-28 of Cycle 1 (cycle length=28 days); Arm D: Days 1-35 of Cycle 1 (cycle length=28 days except for Cycle 1=35 days)
Number of Participants With Adverse Events (AEs)
Baseline up until 30 days following the last administration of study treatment or until initiation of another anti-cancer therapy, whichever occurs first (up to a maximum of 9.25 years).

Secondary Endpoints

Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC[0-inf]) of Docetaxel (Arm A)
Immediately prior to docetaxel infusion, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours (hrs) after start of docetaxel infusion on Day 1 Cycles 1 and 2 (1 cycle=21 days)
Plasma Terminal Half-Life (t1/2) of Docetaxel (Arm A)
Immediately prior to docetaxel infusion, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours (hrs) after start of docetaxel infusion on Day 1 Cycles 1 and 2 (1 cycle=21 days)
Plasma Clearance (CL) of Docetaxel (Arm A)
Immediately prior to docetaxel infusion, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours (hrs) after start of docetaxel infusion on Day 1 Cycles 1 and 2 (1 cycle=21 days)
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Arm A (Doc + Ipat 100mg)EXPERIMENTALParticipants received ipatasertib at a dose of 100 milligrams (mg) once daily for 14 consecutive days (beginning on Day 2) in combination with docetaxel on Day 1, in 21-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm A (Doc + Ipat 200mg)EXPERIMENTALParticipants received ipatasertib at a dose of 200mg once daily for 14 consecutive days (beginning on Day 2) in combination with docetaxel on Day 1, in 21-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm A (Doc + Ipat 400mg)EXPERIMENTALParticipants received ipatasertib at a dose of 400mg once daily for 14 consecutive days (beginning on Day 2) in combination with docetaxel on Day 1, in 21-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm A (Doc + Ipat 600mg)EXPERIMENTALParticipants received ipatasertib at a dose of 600mg once daily for 14 consecutive days (beginning on Day 2) in combination with docetaxel on Day 1, in 21-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm B (mFOLFOX + Ipat 100mg)EXPERIMENTALParticipants received ipatasertib at a dose of 100mg once daily for 7 consecutive days (beginning on Day 1) in combination with mFOLFOX6 chemotherapy (comprising of oxaliplatin, leucovorin, and 5-FU) on Day 1, in 14-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm B (mFOLFOX + Ipat 200mg)EXPERIMENTALParticipants received ipatasertib at a dose of 200mg once daily for 7 consecutive days (beginning on Day 1) in combination with mFOLFOX6 chemotherapy (comprising of oxaliplatin, leucovorin, and 5-FU) on Day 1, in 14-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm B (mFOLFOX + Ipat 400mg)EXPERIMENTALParticipants received ipatasertib at a dose of 400mg once daily for 7 consecutive days (beginning on Day 1) in combination with mFOLFOX6 chemotherapy (comprising of oxaliplatin, leucovorin, and 5-FU) on Day 1, in 14-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm B (mFOLFOX + Ipat 600mg)EXPERIMENTALParticipants received ipatasertib at a dose of 600mg once daily for 7 consecutive days (beginning on Day 1) in combination with mFOLFOX6 chemotherapy (comprising of oxaliplatin, leucovorin, and 5-FU) on Day 1, in 14-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm C (Pac + Ipat 400mg)EXPERIMENTALParticipants received ipatasertib at a dose of 400mg once daily for 21 consecutive days (beginning on Day 1) in combination with paclitaxel on Days 1, 8, and 15, in 28-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm C (Pac + Ipat 600mg)EXPERIMENTALParticipants received ipatasertib at a dose of 600mg once daily for 21 consecutive days (beginning on Day 1) in combination with paclitaxel on Days 1, 8, and 15, in 28-day continuous cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first.
Arm D (Enza + Ipat 400mg)EXPERIMENTALParticipants received ipatasertib at a dose of 400mg once daily alone for 8 days, then from Day 9, ipatasertib will be administered in combination with enzalutamide once daily for 27 days (Cycle 1 duration = 35 days). Participants received both ipatasertib and enzalutamide once daily continuously in subsequent 28-days cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first. Higher (up to 600 mg) or lower dose of ipatasertib may be evaluated in subsequent cycles depending upon safety, tolerability, and pharmacokinetics of the first cycle.
Arm D (Enza + Ipat 600mg)EXPERIMENTALParticipants received ipatasertib at a dose of 600mg once daily alone for 8 days, then from Day 9, ipatasertib will be administered in combination with enzalutamide once daily for 27 days (Cycle 1 duration = 35 days). Participants received both ipatasertib and enzalutamide once daily continuously in subsequent 28-days cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first. Higher (up to 600 mg) or lower dose of ipatasertib may be evaluated in subsequent cycles depending upon safety, tolerability, and pharmacokinetics of the first cycle.
Arm D (Enza + Ipat 400-600mg)EXPERIMENTALParticipants received ipatasertib at a dose of 400-600mg once daily alone for 8 days, then from Day 9, ipatasertib will be administered in combination with enzalutamide once daily for 27 days (Cycle 1 duration = 35 days). Participants received both ipatasertib and enzalutamide once daily continuously in subsequent 28-days cycles, until disease progression, unacceptable toxicity, or use of another anti-cancer therapy, whichever occurred first. Higher (up to 600 mg) or lower dose of ipatasertib may be evaluated in subsequent cycles depending upon safety, tolerability, and pharmacokinetics of the first cycle.

Interventions

NameTypeDescription
5-FUDRUG5-FU at a dose level of 400 mg/m\^2 as intravenous (IV) injection followed by a dose of 2400 mg/m\^2 as IV infusion over 46 hrs will be administered on Day 1 of each 14-day cycle until disease progression or unacceptable toxicity.
DocetaxelDRUGDocetaxel will be administered at dose level of 75 mg/m\^2 as IV infusion over 1 hr on Day 1 of each 21-day cycle until disease progression or unacceptable toxicity.
EnzalutamideDRUGEnzalutamide will be administered orally at a dose level of 160 mg once daily continuously as per schedule defined in respective arm until disease progression or unacceptable toxicity.
IpatasertibDRUGIpatasertib will be administered orally (in escalating doses during Stage 1 followed by at a dose decided during Stage 1) as per schedule defined in the respective arms.
LeucovorinDRUGLeucovorin at a dose level of 400 mg/m\^2 as IV infusion over 2 hrs will be administered on Day 1 of each 14-day cycle until disease progression or unacceptable toxicity.
OxaliplatinDRUGOxaliplatin at a dose level of 85 mg/m\^2 as IV infusion over 2 hours will be administered on Day 1 of each 14-day cycle until disease progression or unacceptable toxicity.
PaclitaxelDRUGPaclitaxel at a dose of 90 mg/m\^2 as IV infusion over 1 hr will be administered on Days 1, 8, and 15 of each 28-day cycle until disease progression or unacceptable toxicity.
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Eligibility Criteria

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

Inclusion Criteria: * Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1 at screening * Histologically or cytologically documented advanced or metastatic solid tumors for which established therapy either does not exist or has proven ineffective or intolerable * Life expectancy g...

Countries:United StatesFranceSpainUnited Kingdom
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Frequently asked questions about Enzalutamide

What is Enzalutamide used for?

Enzalutamide is an investigational small molecule being studied for the treatment of neoplasms, which are abnormal growths of tissue that can be benign or malignant. It is currently in Phase 1 clinical development for this oncology indication.

Who makes Enzalutamide?

Enzalutamide is being developed by Roche Holding AG, a company traded on the OTC market under the ticker symbol RHHBY. The drug is in Phase 1 clinical development for the treatment of neoplasms.

What phase is Enzalutamide in?

Enzalutamide is in Phase 1 clinical development. It is an investigational drug, meaning it has not been approved by regulatory authorities and is still being studied in clinical trials for the treatment of neoplasms.

What clinical trials is Enzalutamide in?

Enzalutamide has been studied in one completed clinical trial, NCT01362374, which evaluated its safety and clinical pharmacology in combination with other agents in participants with advanced solid tumors. The trial enrolled 122 participants and was conducted in the United States, France, Spain, and the United Kingdom.

Is Enzalutamide the same as GDC-0068?

Enzalutamide is not the same as GDC-0068. In the clinical trial NCT01362374, Enzalutamide was studied in combination with GDC-0068, which is a separate investigational drug. Enzalutamide is being developed by Roche Holding AG for the treatment of neoplasms.