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Apitolisib

Phase 1

Prostate Cancer | Small molecule | Oncology |Roche Holding AG|Last Updated: Sep 14, 2023

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials1
Total Enrollment298

FDA Designations

No designations recorded

Clinical trial landscape

Apitolisib · 1 trial · 1 indication

Phase 1 1
NCT01485861Study of Ipatasertib or Apitolisib With Abiraterone Acetate Versus Abiraterone Acetate in Participants With Castration-Resistant Prostate Cancer Previously Treated With Docetaxel ChemotherapyProstate Cancer
COMPLETED298 Analytics
PHASE1COMPLETED
Study of Ipatasertib or Apitolisib With Abiraterone Acetate Versus Abiraterone Acetate in Participants With Castration-Resistant Prostate Cancer Previously Treated With Docetaxel Chemotherapy
Prostate CancerUnlock trial analytics

Study Endpoints

Primary Endpoints

Phase Ib: Percentage of Participants With Dose-Limiting Toxicities (DLTs)
Days 1 to 28 of Cycle 1 (Cycle length = 28 days)

DLT: 1 of the following toxicities, at least possibly related to ipatasertib or apitolisib. 1) Grade ≥ 3 non-hematologic, non-hepatic major organ AE; 2) Grade ≥ 3 febrile neutropenia; 3) Grade ≥ 4 neutropenia (absolute neutrophils less than \[\<\] 500 per microliter) lasting greater than (\>) 7 days; 4) Grade ≥3 thrombocytopenia associated with acute hemorrhage; 5) Grade ≥4 thrombocytopenia; 6) Grade ≥4 anemia; 7) 1 episode of fasting Grade ≥4 hyperglycemia or 3 episodes of fasting Grade 3 hyperglycemia on separate days within 7 days, as determined by laboratory blood glucose evaluation; 8) Grade ≥3 elevation lasting for \> 48 hours for hepatic transaminase or liver-specific alkaline phosphatase or total bilirubin. Adverse events were graded according to the National Cancer Institute Common Terminology Criteria for Adverse Events v 4.0.

Phase Ib: Percentage 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 approximately 10 months).

An Adverse Event (AE) was defined as any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not considered related to the medicinal product.

Phase Ib: Recommended Phase II Dose (RP2D) of Ipatasertib and Apitolisib
Days 1 to 28 of Cycle 1 (Cycle length = 28 days)

RP2D is a dose of a drug which would be used in Phase II stage of the study. RP2D was to be determined based on maximum tolerated dose (MTD) in Phase Ib stage of the study. The highest dose level (in 3+3 escalation scheme) with an acceptable safety profile and with a minimum of 6 participants at which fewer than one-third of participants experienced a DLT was declared the MTD and RP2D.

Phase II: Radiographic Progression Free Survival (rPFS) (Intent-To-Treat [ITT] Population)
Screening up to radiographic progression or death, whichever occurred first (assessed at screening, after Cycles 3, 5, 7, 9, every three cycles [12 weeks] thereafter up to end of treatment [up to 3.6 years overall]) (cycle length = 28 days)

rPFS: Time from randomization to the first occurrence of disease progression, as determined by investigator review of tumor assessments via CT scan and bone scans, or death on study from any cause, whichever occurred first. Progression was defined as follows: Soft tissue mass (Response Evaluation Criteria in Solid Tumors \[RECIST\] 1.1): at least 20% increase in sum of diameters of target lesions compared to smallest sum of diameters on-study and absolute increase of at least 5 mm, progression of existing non-target lesions, or presence of new lesions. Bone: ≥ 2 new bone lesions plus 2 additional at confirmation on a second bone scan ≥ 4 weeks later (\< 12 weeks after randomization). ≥ 2 new bone lesions consistent with progression, without need for confirmatory bone scan (≥ 12 weeks after randomization).

Phase II: rPFS in Participants With Institute of Cancer Research (ICR) Phosphatase and Tensin Homolog (PTEN) Loss
Screening up to radiographic progression or death, whichever occurred first (assessed at screening, after Cycles 3, 5, 7, 9, every three cycles [12 weeks] thereafter up to end of treatment [up to 3.6 years overall]) (cycle length = 28 days)

rPFS: Time from randomization to the first occurrence of disease progression, as determined by investigator review of tumor assessments via CT scan and bone scans, or death on study from any cause, whichever occurred first. Progression was defined as follows: Soft tissue mass (RECIST 1.1): at least 20% increase in sum of diameters of target lesions compared to smallest sum of diameters on-study and absolute increase of at least 5 mm, progression of existing non-target lesions, or presence of new lesions. Bone: ≥ 2 new bone lesions plus 2 additional at confirmation on 2nd bone scan ≥ 4 weeks later (\< 12 weeks after randomization). ≥ 2 new bone lesions consistent with progression, without need for confirmatory bone scan (≥ 12 weeks after randomization). PTEN status was assessed by RUO IHC assay that was performed at ICR, UK. Samples with 100% of the tumor with no PTEN staining were classified as "ICR PTEN loss". Number of participants analyzed=participants with PTEN loss.

Secondary Endpoints

Phase Ib: Maximum Plasma Concentration (Cmax) of Ipatasertib When Co-Administered With Abiraterone
Pre-dose (0 hour), 1, 2, 4, 6, 24 hours post dose on Days 1, 15 of Cycle 1 (cycle length = 28 days)
Phase Ib: Time to Cmax (Tmax) of Ipatasertib When Co-Administered With Abiraterone
Pre-dose (0 hour), 1, 2, 4, 6, 24 hours post dose on Days 1, 15 of Cycle 1 (cycle length = 28 days)
Phase Ib: Area Under The Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24) of Ipatasertib When Co-Administered With Abiraterone
Pre-dose (0 hour), 1, 2, 4, 6, 24 hours post dose on Days 1, 15 of Cycle 1 (cycle length = 28 days)
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Phase Ib: Ipatasertib 400 mg + abirateroneEXPERIMENTALParticipants will receive ipatasertib 400 mg once daily, abiraterone 1000 mg once daily, and prednisone/prednisolone 5 mg twice daily (bid) continuously in 28-day treatment cycles until disease progression or intolerable toxicity.
Phase Ib: Apitolisib 30 mg + abirateroneEXPERIMENTALParticipants will receive apitolisib 30 mg once daily, abiraterone 1000 mg once daily, and prednisone/prednisolone 5 mg twice daily (bid) continuously in 28-day treatment cycles until disease progression or intolerable toxicity.
Phase II: Ipatasertib 400 mg + abirateroneEXPERIMENTALParticipants will receive Ipatasertib 400 mg once daily, abiraterone 1000 mg once daily, and prednisone/prednisolone 5 mg bid continuously in 28-day treatment cycles until disease progression or intolerable toxicity.
Phase II: Ipatasertib 200 mg + abirateroneEXPERIMENTALParticipants will receive Ipatasertib 200 mg once daily, abiraterone 1000 mg once daily, and prednisone/prednisolone 5 mg bid continuously in 28-day treatment cycles until disease progression or intolerable toxicity.
Phase II: Placebo + abirateronePLACEBO_COMPARATORParticipants will receive placebo (for Ipatasertib) once daily, abiraterone 1000 mg once daily, and prednisone/prednisolone 5 mg bid continuously in 28-day treatment cycles until disease progression or intolerable toxicity.
Safety Cohort: Ipataseritib 400 mg + Abiraterone + PrednisoneEXPERIMENTALParticipants will receive ipatasertib 400 mg orally once daily and/or prednisone/prednisolone 5 mg orally once daily or bid and/or abiraterone 1000 mg orally once daily according to the following schedule: ipatasertib in the morning during Cycle 1, Days 1-7; ipatasertib in the morning plus prednisone/prednisolone once at night during Cycle 1, Day 8; ipatasertib in the morning plus prednisone/prednisolone bid (morning and night) during Cycle 1, Days 9-11; ipatasertib in the morning plus prednisone/prednisolone bid (morning and night) and abiraterone in the morning during Cycle 1, Days 12-18; ipatasertib in the evening plus prednisone/prednisolone bid (morning and night) and abiraterone at the same time as ipatasertib during Cycle 1, Days 19-25; Cycle 2 and beyond ipatasertib once daily in the morning or evening, abiraterone at the same time as ipatasertib, and prednisone/prednisolone bid.

Interventions

NameTypeDescription
AbirateroneDRUGOrally once daily
ApitolisibDRUGOrally once daily
IpatasertibDRUGOrally once daily
PlaceboDRUGOrally once daily
PrednisoneDRUGOrally bid
PrednisoloneDRUGOrally bid
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Eligibility Criteria

Age Range18 Years to N/A
SexMALE
Healthy VolunteersNo
Study Sites59

Inclusion Criteria: * Histologically confirmed metastatic or advanced prostate adenocarcinoma that has been previously treated with docetaxel-based therapy and has progressed during treatment of at least one hormonal therapy(prior docetaxel is not required for the safety cohort) * Two rising PSA le...

Countries:United StatesCzechiaFranceGreeceItalyNetherlandsRomaniaSpainUnited Kingdom
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Competitive Landscape -Prostate Cancer 254 trials

Frequently asked questions about Apitolisib

What is Apitolisib used for in prostate cancer?

Apitolisib is an investigational small molecule being studied for the treatment of castration-resistant prostate cancer in patients previously treated with docetaxel chemotherapy. It is being evaluated in combination with abiraterone acetate compared to abiraterone acetate alone. The drug is still in clinical development and is not approved.

What does Apitolisib target?

Apitolisib is a small molecule that inhibits both PI3K and mTOR kinases, which are key components of the PI3K/AKT/mTOR signaling pathway involved in cell growth and survival. By blocking these targets, Apitolisib aims to reduce tumor cell proliferation in prostate cancer.

Who is developing Apitolisib?

Apitolisib is being developed by Roche Holding AG, which trades under the ticker RHHBY. The company is conducting clinical trials to evaluate the drug's safety and efficacy in prostate cancer.

What phase is Apitolisib in?

Apitolisib is in Phase 1 clinical development. The drug is investigational and has not been approved by regulatory authorities. It is being studied in a completed Phase 1 trial for castration-resistant prostate cancer.

What clinical trials is Apitolisib in?

Apitolisib was studied in a Phase 1 clinical trial with the identifier NCT01485861. This completed trial enrolled 298 participants with castration-resistant prostate cancer previously treated with docetaxel chemotherapy. The study was conducted across multiple countries including the United States, Czechia, France, Greece, Italy, Netherlands, Romania, Spain, and the United Kingdom.

Is Apitolisib the same as Ipatasertib?

No, Apitolisib is not the same as Ipatasertib. They are two distinct investigational drugs being studied in the same clinical trial. The trial compared either Ipatasertib or Apitolisib combined with abiraterone acetate against abiraterone acetate alone in patients with castration-resistant prostate cancer.