Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as GCD-0032, GDC-0032
Taselisib · 3 trials · 4 indications
Objective response rate (ORR) was defined as proportion of participants achieving complete response (CR) or partial response (PR). As per modified RECIST v1.1, CR: disappearance of all target lesions, PR: at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum of diameters.
Total pCR was assessed by local pathology review on samples taken at surgery following completion of neoadjuvant therapy. tpCR was defined as the absence of any residual invasive cancer on hematoxylin and eosin evaluation of the resected breast specimen and all sampled ipsilateral lymph nodes ( i.e., ypT0/Tis, ypN0 in the AJCC staging system, 7th edition).
ORR was defined as proportion of participants achieving CR or PR. As per modified RECIST v1.1, CR: disappearance of all target lesions, PR: at least a 30% decrease in the sum of diameters of target lesions, taking as reference the baseline sum of diameters.
Total pCR was assessed by local pathology review on samples taken at surgery following completion of neoadjuvant therapy. tpCR was defined as the absence of any residual invasive cancer on hematoxylin and eosin evaluation of the resected breast specimen and all sampled ipsilateral lymph nodes (i.e., ypT0/Tis, ypN0 in the AJCC staging system, 7th edition).
| Arm | Type | Description |
|---|---|---|
| Letrozole + Placebo | PLACEBO_COMPARATOR | Participants will receive 2.5 mg letrozole tablets orally QD along with placebo on a 5-days-on/2-days-off schedule for a total of 16 weeks. |
| Letrozole + Taselisib | EXPERIMENTAL | Participants will receive 2.5 milligrams (mg) letrozole tablets orally once daily (QD) along with taselisib tablets at 4 mg (two 2 mg tablets) orally on a 5 days-on/2 days-off schedule for a total of 16 weeks. |
| Arm A | EXPERIMENTAL | Arm A \- Taselisib with Trastuzumab emtansine (also called T-DM1) * Taselisib administered orally, daily in each treatment cycle (3 weeks). * Trastuzumab emtansine (also called T-DM1) administered once via IV per treatment cycle (3 weeks). |
| Arm B | EXPERIMENTAL | Arm B -Taselisib with T-DM1 and Pertuzumab * Taselisib is administered oral, daily or every other day per treatment cycle (3 weeks). * Trastuzumab emtansine (also called T-DM1) administered once via IV per treatment cycle (3 weeks). * Pertuzumab- administered once via IV per treatment cycle (3 weeks). |
| Arm C | EXPERIMENTAL | Arm C: * Taselisib with Pertuzumab and Trastuzumab * Cohort C will not open without additional authorization from Genentech * Taselisib is administered oral, daily in each treatment cycle (3 weeks). * Trastuzumab administered once via IV per treatment cycle (3 weeks). * Pertuzumab- administered once via IV per treatment cycle (3 weeks). |
| Arm D | EXPERIMENTAL | Arm D * Taselisib with Pertuzumab, Trastuzumab, and Paclitaxel * Cohort will not be opened without additional authorization from Genentech * Taselisib- administered oral, daily in each treatment cycle (3 weeks). * Pertuzumab- administered once via IV per treatment cycle (3 weeks). * Trastuzumab administered once via IV per treatment cycle (3 weeks). * Paclitaxel- administered via IV, weekly for 3 weeks within each cycle. |
| Arm A: GDC-0032 + Docetaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily for 21 consecutive days (beginning from Day 1) in each 21-day cycle along with Docetaxel on Day 1 of each 21-day cycle. |
| Arm B: GDC-0032 + Paclitaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily for 28 consecutive days (beginning from Day 1) in each 28-day cycle along with Paclitaxel on Days 1, 8, 15 and 22 of each 28-day cycle. |
| Arm C: GDC-0032 + Docetaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily on Day 1 and Days 8-14 of each 21-day cycle along with Docetaxel on Day 1 of each 21-day cycle. |
| Arm D: GDC-0032 + Docetaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily on Days 2-14 of each 21-day cycle along with Docetaxel on Day 1 of each 21-day cycle. |
| Arm E: GDC-0032 + Docetaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily on Days 1-14 of each 21-day cycle along with Docetaxel on Day 1 of each 21-day cycle. |
| Arm F: GDC-0032 + Paclitaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily on a 5-days on, 2-days off schedule in each 28-day cycle along with Paclitaxel on Days 1, 8, 5 and 22 of each 28-day cycle. |
| Arm G: GDC-0032 + Paclitaxel | EXPERIMENTAL | Participants will receive GDC-0032 once daily on a 3-days on, 4-days off schedule in each 28-day cycle along with Paclitaxel on Days 1, 8, 5 and 22 of each 28-day cycle. |
| Name | Type | Description |
|---|---|---|
| Letrozole | DRUG | Letrozole tablets will be administered orally at 2.5 mg QD for 16 weeks. |
| Placebo | OTHER | Placebo tablets matched to taselisib formulation will be administered orally daily on 5 days-on/2 days-off schedule for up to 16 weeks. |
| Taselisib | DRUG | Taselisib will be administered orally at 4 mg (two 2 mg tablets) daily. |
| Trastuzumab emtansine | DRUG | - |
| Pertuzumab | DRUG | - |
| Trastuzumab | DRUG | - |
| Paclitaxel | DRUG | - |
| Docetaxel | DRUG | Participants will receive docetaxel 75 milligrams per meter-squared (mg/m\^2) intravenous (IV) dose on Day 1 of each 21-day cycle. |
| GDC-0032 | DRUG | Participants will receive escalated dose of GDC-0032. The initial dose will be 3 mg capsules or 2 mg tablets. |
Inclusion Criteria: * Female participants * Postmenopausal status * Histologically confirmed invasive breast carcinoma, with all of the following characteristics: (i) Primary tumor greater than or equal to (\>/=) 2 centimeters (cm) in largest diameter (cT1-3) by MRI; (ii) Stage I to operable Stage ...
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Taselisib is an investigational small molecule being studied for the treatment of breast cancer, including metastatic and recurrent breast cancer. It has been evaluated in both early and advanced breast cancer settings, including a neoadjuvant study in post-menopausal women with breast cancer and a study in advanced HER2-positive breast cancer.
Taselisib targets multiple phosphoinositide 3-kinase (PI3K) isoforms, specifically PIK3CA, PIK3CB, PIK3CD, PIK3CG, PIK3R1, and PIK3R2. It acts as an inhibitor of these targets. This mechanism is relevant to breast cancer, where PI3K pathway alterations are common, and trials have used biomarker selection to identify appropriate patients.
Taselisib is being developed by Roche Holding AG, which trades on the OTC market under the ticker RHHBY. Roche conducted the clinical development program for the drug, including the Phase 2 LORELEI study and a Phase 1b dose-escalation trial in advanced HER2-positive breast cancer.
Taselisib is in Phase 2 clinical development. It is an investigational agent and has not been approved by the FDA. The Phase 2 program includes the LORELEI trial, which evaluated neoadjuvant letrozole plus taselisib versus letrozole plus placebo in post-menopausal women with breast cancer.
Taselisib has been studied in two completed clinical trials. NCT02273973, known as LORELEI, was a Phase 2 randomized, double-blind, placebo-controlled study of neoadjuvant letrozole plus taselisib versus letrozole plus placebo in 334 post-menopausal women with breast cancer across multiple countries. NCT02390427 was a Phase 1b dose-escalation trial of taselisib in combination with anti-HER2 therapies in 68 participants with advanced HER2-positive breast cancer in the United States.
Yes, Taselisib is also known as GDC-0032. The Phase 1b dose-escalation trial NCT02390427 refers to the drug as Taselisib (GDC-0032), confirming that both names identify the same investigational PI3K inhibitor developed by Roche for breast cancer.