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Also known as LY4064809, STX-478
Tersolisib · 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...
Tersolisib is an investigational small molecule drug being developed by Eli Lilly and Company under the ticker LLY. It is in Phase 1 clinical development. Its therapeutic indications have not been disclosed, and it is identified in company materials as LY4064809.
Tersolisib targets phosphoinositide 3-kinase, or PI3K. The drug belongs to the -lisib class of PI3K inhibitors, a group of small molecules that act on this lipid kinase pathway. Its specific PI3K isoform selectivity has not been disclosed.
Tersolisib is being developed by Eli Lilly and Company, which trades on the New York Stock Exchange under the ticker LLY. Lilly is the sole sponsor listed for the clinical program, and the compound also carries the internal designation LY4064809.
Tersolisib is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA. The Phase 1 program to date consists of one completed trial, with no active trials currently listed.
Tersolisib has been studied in one Phase 1 trial, NCT07662798, titled A Study of Food Effect on Tersolisib (LY4064809) in Healthy Participants. That trial is completed, enrolled 60 healthy volunteers in the United States, and used a controlled, randomized design without blinding.
Yes. Tersolisib is the same compound as LY4064809. LY4064809 is Eli Lilly's internal alphanumeric designation for the molecule, while Tersolisib is its international nonproprietary name. Both names refer to the same investigational PI3K-targeted small molecule.