Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Apitolisib · 1 trial · 1 indication
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.
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.
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.
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).
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.
| Arm | Type | Description |
|---|---|---|
| Phase Ib: Ipatasertib 400 mg + abiraterone | EXPERIMENTAL | Participants 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 + abiraterone | EXPERIMENTAL | Participants 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 + abiraterone | EXPERIMENTAL | Participants 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 + abiraterone | EXPERIMENTAL | Participants 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 + abiraterone | PLACEBO_COMPARATOR | Participants 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 + Prednisone | EXPERIMENTAL | Participants 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. |
| Name | Type | Description |
|---|---|---|
| Abiraterone | DRUG | Orally once daily |
| Apitolisib | DRUG | Orally once daily |
| Ipatasertib | DRUG | Orally once daily |
| Placebo | DRUG | Orally once daily |
| Prednisone | DRUG | Orally bid |
| Prednisolone | DRUG | Orally bid |
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...
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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.
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.
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.
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.
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.
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.