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Also known as [14C]-STX-478, LY4064809, Tersolisib, LY4064809 Test Formulation, LY4064809 Reference Formulation
STX-478 · 3 trials · 5 indications
As determined by the investigator based on Response Evaluation Criteria in Solid Tumors (RECIST) v 1.1
Investigator-assessed
| Arm | Type | Description |
|---|---|---|
| LY4064809 + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 1) | EXPERIMENTAL | LY4064809 given orally in one of two doses in combination with investigator's choice of CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| LY4064809 + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 2) | EXPERIMENTAL | LY4064809 given orally in combination with CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| Placebo + CDK4/6 Inhibitor + Endocrine Therapy (ET) (Part 2) | PLACEBO_COMPARATOR | Placebo given orally in combination with CDK4/6 inhibitor given orally and ET given orally or intramuscularly |
| Group 1 Treatment A Fasted | EXPERIMENTAL | Tersolisib administered orally. |
| Group 1 Treatment B High-Fat Meal | EXPERIMENTAL | Tersolisib administered orally. |
| Group 2 Treatment A Fasted | EXPERIMENTAL | Tersolisib administered orally. |
| Group 2 Treatment C Low-Fat Meal | EXPERIMENTAL | Tersolisib administered orally. |
| Dose Escalation (Advanced Solid Tumors) | EXPERIMENTAL | * Cohort A0: Advanced Solid tumors expressing PI3Kα mutations * Cohort A1: HR+ breast cancer expressing PI3Kα mutations |
| Dose Expansion | EXPERIMENTAL | * Cohort A2: Gynecologic cancers * Cohort A3: Head and Neck Squamous Cell Carcinoma * Cohorts A4/A5: Other solid tumors not included in Cohorts A1, A2, A3 expressing PI3Kα mutations * Cohort A6: Endometrial cancer * Cohort A7: Non-gastrointestinal solid tumors |
| Dose Selection/Expansion: Combination STX-478 + fulvestrant | EXPERIMENTAL | Cohort B: HR+/HER2- or HR+/HER2low breast cancer expressing PI3Kα mutations |
| Dose Selection/Expansion Combination | EXPERIMENTAL | STX-478 + Endocrine therapy + CDK4/6 inhibitor Cohort C/D/E: HR+/HER2- or HR+/HER2low breast cancer expressing PI3Ka mutations |
| Experimental: Drug to Drug Interaction (DDI) Metformin STX-478 +/- ET ([AIs or fulvestrant] | EXPERIMENTAL | CDK4/6 inhibitor therapy in Cohort A8: all solid tumors Cohort B2 and Cohort F: HR+/HER2- or HR+/HER2 low breast cancer expressing PI3Kα mutations |
| Name | Type | Description |
|---|---|---|
| LY4064809 | DRUG | Administered orally |
| Placebo | DRUG | Administered orally |
| Ribociclib | DRUG | Administered orally |
| Palbociclib | DRUG | Administered orally |
| Abemaciclib | DRUG | Administered orally |
| Anastrozole | DRUG | Administered orally |
| Letrozole | DRUG | Administered orally |
| Exemestane | DRUG | Administered orally |
| Fulvestrant | DRUG | Administered intramuscular |
| Tersolisib | DRUG | Tersolisib administered orally |
| High-fat Meal | OTHER | High-fat Meal |
| Low-fat Meal | OTHER | Low-fat Meal |
| STX-478 | DRUG | STX-478 is a mutant-selective PI3Kα inhibitor |
| Tamoxifen | DRUG | Tamoxifen |
| Imlunestrant | DRUG | Imlunestrant |
| Metformin | DRUG | Metformin |
Inclusion Criteria: * Are willing to follow contraception requirements. Contraceptive use by participants should be consistent with local regulations regarding the methods of contraception for those participating in clinical trials. * If assigned female at birth, pre-/peri- and postmenopausal statu...
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STX-478 is an investigational small molecule being studied in adults with advanced solid tumors, including breast cancer. It is being evaluated as monotherapy and in combination with other antineoplastic agents in a Phase 1 first-in-human study. It is not approved for any indication and remains in clinical development.
STX-478 targets PIK3CA, the gene encoding the p110 alpha catalytic subunit of phosphatidylinositol 3-kinase. PIK3CA is a commonly altered gene in several cancers, including breast cancer, and is the molecular target of this small molecule agent.
STX-478 is being developed by Eli Lilly and Company, which trades on the New York Stock Exchange under the ticker LLY. Lilly is the sponsor of the ongoing Phase 1 first-in-human study of STX-478 in advanced solid tumors.
STX-478 is in Phase 1 clinical development. The single registered trial is a first-in-human Phase 1 study that is currently recruiting participants. STX-478 is investigational and has not been approved by the FDA or any other regulatory agency for any indication.
STX-478 is being studied in one active trial, NCT05768139, titled a first-in-human study of tersolisib (STX-478) as monotherapy and in combination with other antineoplastic agents in participants with advanced solid tumors. The trial is recruiting, with an estimated enrollment of 880 participants across the United States, Belgium, France, Germany, Ireland, Italy, Japan, the Netherlands, and Spain.
Yes, [14C]-STX-478 is an alternative name for STX-478, referring to the carbon-14 labeled form of the compound used in research. STX-478 is also known as tersolisib, the name used in its clinical trial title.