Evaluation of the Pharmacokinetics, Safety, and Tolerability of IM Letrozole LEBE in Healthy Post-menopausal Women

What this trial studies

This is a Phase I, open label, sequential, single ascending dose (SAD) study to evaluate the pharmacokinetic (PK), safety, and tolerability of Letrozole LEBE in healthy post-menopausal women.

Conditions in scope

• Healthy

Interventions

• Letrozole LEBE 75 mg (Drug) — 14 oral doses of Femara 2.5 mg/daily + 28-days (at least) washout period + single IM injection of Letrozole LEBE 75 mg
• Letrozole LEBE 150 mg (Drug) — 14 oral doses of Femara 2.5 mg/daily + 28-days (at least) washout period + single IM injection of Letrozole LEBE 150 mg
• Letrozole LEBE 225 mg (Drug) — 14 oral doses of Femara 2.5 mg/daily + 28-days (at least) washout period + single IM injection of Letrozole LEBE 225mg

Who can join

Women only · Ages 18 Years to 75 Years · Accepts healthy volunteers.

Inclusion criteria

• Healthy post-menopausal women.
• Capable of providing informed consent.
• Weight of ≥50 kg and a BMI ≥19 and ≤39 kg/m2.
• Subjects should be able to communicate with clinic staff.

Exclusion criteria

• Subjects who have a history of allergy or hypersensitivity to letrozole or any of the inactive ingredients.
• Subjects who have a history of galactose intolerance, severe hereditary lactase deficiency glucose-galactose malabsorption.
• Subjects who have used estrogen or progesterone hormone replacement therapy, thyroid replacement therapy, oral contraceptives, androgens, luteinizing hormone (LH) releasing hormone analogs, prolactin inhibitors, or antiandrogens within prior to Screening.
• Subjects who have used: any medications including St. John's wort or any medications or products known to be potent or moderate inhibitors of CYP P450 3A4.
• Subjects who have been diagnosed with osteoporosis.
• Subjects who have an abnormality at Screening or prior to first dose that in the opinion of the investigator increases the risk of participating in the study.
• Subjects who have any clinically significant abnormal physical examination or laboratory safety findings at screening.
• Subjects who have relevant diseases or clinically significant abnormal relevant findings at Screening, as determined by medical history, physical examination, laboratory, ECG, DEXA, and breast and pelvic examination.

Eligibility wording paraphrased from the public record. View the full criteria on ClinicalTrials.gov before contacting a site.

Where it’s happening

Status & timeline

• Overall status: Active, not recruiting
• Study type: Interventional
• Phase: PHASE1
• Start date: 2023-07-26
• Primary completion: 2026-03
• Last update posted: 2026-03-04
• First posted: 2024-03-18

Sponsor & contact

Lead sponsor: Rovi Pharmaceuticals Laboratories (Industry)

For trial site contact information, use the official record at ClinicalTrials.gov. Contact details change frequently and the public record is the source of truth.

Outcome measures

Primary outcomes

• λz (Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197)
  Terminal phase elimination rate constant
• Cmax (Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197)
  Maximum observed plasma concentration after Letrozole LEBE administration
• Clast (Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197)
  Last observed plasma concentration after Letrozole LEBE administration
• tmax (Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197)
  Time to maximum observed concentration
• tlag (Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197)
  Lag time before observation of quantifiable concentrations in plasma.

Related ClearedRx care

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