Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Imlunestrant · 6 trials · 4 indications
IDFS excluding second non-breast primary invasive cancers
PFS was defined as the time from randomization to the date of first documented progression of disease or death from any cause in the absence of disease progression using Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 criteria, as assessed by investigator. Progressive disease (PD) was defined as at least a 20% increase in the sum of the diameters of target lesions, with reference being the smallest sum on study and an absolute increase of at least 5 mm, or unequivocal progression of non-target lesions, or 1 or more new lesions. Participants known to be alive and without disease progression were censored at the date of their last adequate tumor assessment per RECIST 1.1 criteria, or date of randomization (whichever is later).
PFS was defined as the time from randomization to the date of first documented progression of disease or death from any cause in the absence of disease progression using Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 criteria, as assessed by investigator. Progressive disease (PD) was defined as at least a 20% increase in the sum of the diameters of target lesions, with reference being the smallest sum on study and an absolute increase of at least 5 mm, or unequivocal progression of non-target lesions, or 1 or more new lesions. Participants known to be alive and without disease progression were censored at the date of their last adequate tumor assessment per RECIST 1.1 criteria, or date of randomization (whichever is later).
PFS was defined as the time from randomization to the date of first documented progression of disease or death from any cause in the absence of disease progression using Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1 criteria, as assessed by investigator. Progressive disease (PD) was defined as at least a 20% increase in the sum of the diameters of target lesions, with reference being the smallest sum on study and an absolute increase of at least 5 mm, or unequivocal progression of non-target lesions, or 1 or more new lesions. Participants known to be alive and without disease progression were censored at the date of their last adequate tumor assessment per RECIST 1.1 criteria, or date of randomization (whichever is later).
PK: AUC\[0-∞\] of Midazolam
PK: Cmax of Midazolam
PK: AUC\[0-∞\] of Repaglinide
PK: Cmax of Repaglinide
PK: AUC\[0-∞\] of Omeprazole
PK: Cmax of Omeprazole
5-hydroxyomeprazole is a major metabolite of omeprazole.
5-hydroxyomeprazole is a major metabolite of omeprazole.
PK: AUC\[0-∞\] of Dextromethorphan
PK: Cmax of Dextromethorphan
Dextrorphan is a major metabolite of Dextromethorphan.
Dextrorphan is a major metabolite of Dextromethorphan.
PK: AUC\[0-∞\] of Imlunestrant
PK: Cmax of Imlunestrant
PK: AUC\[0-∞\] of Rosuvastatin
PK: Cmax of Rosuvastatin
PK: AUC\[0-∞\] of Digoxin
PK: Cmax of Digoxin
PK: Cmax of Imlunestrant is reported.
AUC(0-t) of Imlunestrant is reported.
| Arm | Type | Description |
|---|---|---|
| Imlunestrant | EXPERIMENTAL | Imlunestrant administered orally. |
| Investigator's Choice of Endocrine Therapy | ACTIVE_COMPARATOR | Investigator's choice of tamoxifen, anastrozole, letrozole, or exemestane administered per local approved label. |
| Arm A: Imlunestrant | EXPERIMENTAL | Participants received Imlunestrant 400 milligrams (mg) orally once daily on days 1 to 28 of a 28-day cycle, until disease progression or a criterion for discontinuation were met. |
| Arm B: Investigator's Choice of Endocrine Therapy | EXPERIMENTAL | Participants received the investigator's choice of endocrine therapy, either exemestane 25 mg administered orally once daily on days 1 to 28 of a 28-day cycle, or Fulvestrant 500 mg intramuscularly on days 1 and 15 of Cycle 1, then on Day 1 of Cycle 2 and beyond, until disease progression or a criterion for discontinuation was met. |
| Arm C: Imlunestrant + Abemaciclib | EXPERIMENTAL | Participants received Imlunestrant 400 mg orally once daily on Days 1 to 28 of a 28-day cycle, plus Abemaciclib 150 mg orally twice daily on Days 1 to 28 of a 28-day cycle, until disease progression or a criterion for discontinuation was met. |
| Cohort 1 Arm A | EXPERIMENTAL | Imlunestrant will be given orally |
| Cohort 1 Arm B - Imlunestrant + Goserelin | EXPERIMENTAL | Imlunestrant will be given orally and goserelin will be given subcutaneously (SC) |
| Cohort 1 Arm C - Tamoxifen | ACTIVE_COMPARATOR | Tamoxifen will be given orally |
| Cohort 2 Arm A - Imlunestrant | EXPERIMENTAL | Imlunestrant will be given orally |
| Cohort 2 Arm B - Tamoxifen | ACTIVE_COMPARATOR | Tamoxifen will be given orally |
| Midazolam + Imlunestrant | EXPERIMENTAL | Participants received 400 milligram (mg) Imlunestrant (2 × 200 mg) tablets administered once daily (QD) orally for 7 days on Days 3 to 9 and a single dose of 0.5 mg midazolam solution orally on Day 1 and Day 9 as per below dosing sequence: Day 1: 0.5 mg midazolam alone Days 3 to 8: 400 mg imlunestrant QD alone Day 9: 0.5 mg midazolam + 400 mg imlunestrant There was a washout period of 8 days between doses of midazolam. |
| Imlunestrant + Repaglinide (Cohort 1) | EXPERIMENTAL | Participants received: Day 1: A single oral dose of 0.5 mg repaglinide administered alone. Day 3: A single oral dose of 800 mg imlunestrant, followed approximately 2 hours later by 0.5 mg repaglinide, both administered orally. |
| mlunestrant + Omeprazole & Dextromethorphan (Cohort 2) | EXPERIMENTAL | Participants received: Day 1: A single oral dose of 20 mg omeprazole and 30 mg dextromethorphan, administered in the morning. Day 3: A single oral dose of 800 mg imlunestrant, followed immediately by 20 mg omeprazole and 30 mg dextromethorphan, all administered orally. |
| Imlunestrant + Quinidine (Cohort 3) | EXPERIMENTAL | Participants received: Day 1: A single oral dose of 400 mg imlunestrant, administered in the morning. Days 15 to 17 and 19 to 24: Twice-daily oral doses of 200 mg quinidine, administered alone. Day 18: A single oral dose of 400 mg imlunestrant administered in combination with 200 mg quinidine (quinidine was dosed twice on this day as part of the regular regimen). |
| Imlunestrant + Rosuvastatin & Digoxin (Cohort 4) | EXPERIMENTAL | Participants received: Day 1: A single oral dose of 10 mg rosuvastatin and 0.25 mg digoxin, administered in the morning. Day 10: A single oral dose of 400 mg imlunestrant, administered in combination with 10 mg rosuvastatin and 0.25 mg digoxin, all administered orally. |
| Imlunestrant (Normal Hepatic Function) | EXPERIMENTAL | Participants received a single dose of Imlunestrant 400 milligrams (mg) administered orally on Day 1 in fasted state. |
| Imlunestrant (Mild Hepatic Impairment) | EXPERIMENTAL | Participants received a single dose of Imlunestrant 400 mg administered orally on Day 1 in fasted state. |
| Imlunestrant (Moderate Hepatic Impairment) | EXPERIMENTAL | Participants received a single dose of Imlunestrant 400 mg administered orally on Day 1 in fasted state. |
| Imlunestrant (Severe Hepatic Impairment) | EXPERIMENTAL | Participants received a single dose of Imlunestrant 200 mg administered orally on Day 1 in fasted state. |
| Name | Type | Description |
|---|---|---|
| Imlunestrant | DRUG | Administered orally. |
| Tamoxifen | DRUG | Administered per local approved label. |
| Anastrozole | DRUG | Administered per local approved label. |
| Letrozole | DRUG | Administered per local approved label. |
| Exemestane | DRUG | Administered per local approved label. |
| Fulvestrant | DRUG | Administered IM. |
| Abemaciclib | DRUG | Administered orally. |
| Goserelin | DRUG | Given SC |
| Tamoxifen 20 mg | DRUG | Given orally |
| Midazolam | DRUG | Administered orally. |
| Repaglinide | DRUG | Administered orally. |
| Omeprazole | DRUG | Administered orally. |
| Dextromethorphan | DRUG | Administered orally. |
| Quinidine | DRUG | Administered orally. |
| Rosuvastatin | DRUG | Administered orally. |
| Digoxin | DRUG | Administered orally. |
Inclusion Criteria: * Have a diagnosis of ER+, HER2- early-stage, resected, invasive breast cancer without evidence of distant metastasis. * Participants must have received at least 24 months but not more than 60 months of any adjuvant ET, from time of adjuvant ET initiation. * Participants may hav...
Imlunestrant is an investigational small molecule being studied for the treatment of breast cancer, specifically in patients with estrogen receptor-positive (ER+), HER2-negative advanced or early breast cancer. It is also being evaluated in healthy participants and in individuals with hepatic insufficiency. The drug is currently in Phase 3 clinical development.
Imlunestrant targets the estrogen receptor as a selective estrogen receptor degrader (SERD). By degrading the estrogen receptor, it aims to block estrogen signaling that drives the growth of ER+ breast cancer cells. This mechanism is being studied in both advanced and early breast cancer settings.
Imlunestrant is being developed by Eli Lilly and Company, a pharmaceutical company listed on the New York Stock Exchange under the ticker symbol LLY. The company is conducting multiple clinical trials to evaluate the drug's safety and efficacy in breast cancer and other conditions.
Imlunestrant is in Phase 3 clinical development for breast cancer. It is also being studied in earlier-phase trials, including a Phase 1 study in healthy participants and a Phase 2 study in premenopausal women with early breast cancer. The drug is investigational and not yet approved by regulatory authorities.
Imlunestrant is being evaluated in several clinical trials. NCT04975308 is a Phase 3 study in ER+, HER2- advanced breast cancer. NCT05514054 is a Phase 3 study in early breast cancer. NCT05444556 is a Phase 1 study in healthy female participants, and NCT07287098 is a Phase 2 study in premenopausal women with early breast cancer.
Yes, Imlunestrant is also known as LY3484356. Clinical trial records refer to the drug by both names, with LY3484356 serving as the investigational compound identifier used by Eli Lilly and Company in study documentation.