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

NCT06315205 | Active Not Recruiting Phase 1 DMC

• 2 other identifiers: ROV-LEBE-2023-012023-503948-13
• Study Type: interventional
• Target: 90
• Locations: 1 country
• Sites: 1

Brief Summary

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

Healthy

Keywords

Pharmacokinetics; Safety; Letrozol LEBE; Intramuscular; Breast cancer

Outcome Measures

Primary Outcomes (8)

• λz

  Terminal phase elimination rate constant

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• Cmax

  Maximum observed plasma concentration after Letrozole LEBE administration

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• Clast

  Last observed plasma concentration after Letrozole LEBE administration

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• tmax

  Time to maximum observed concentration

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• tlag

  Lag time before observation of quantifiable concentrations in plasma.

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• t1/2

  Terminal elimination half life.

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• AUC∞

  Area under the concentration time curve from time zero extrapolated to infinity.

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• AUClast

  Area under the concentration time curve from time zero up to the last quantifiable concentration.

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

Secondary Outcomes (10)

• E1

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• SE1

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• E2

  Following single IM administration of Letrozole LEBE (Treatment Period 2, Day 1) until Day 197

• λz

  Following multiple oral administration of Femara (Treatment Period 1, Day 14)

• Cav

  Following multiple oral administration of Femara (Treatment Period 1, Day 14)

Study Arms (3)

Cohort 1: Letrozol LEBE 75 mg

EXPERIMENTAL

Drug: Letrozole LEBE 75 mg

Cohort 2: Letrozol LEBE 150 mg

EXPERIMENTAL

Drug: Letrozole LEBE 150 mg

Cohort 3: Letrozol LEBE 225 mg

EXPERIMENTAL

Drug: Letrozole LEBE 225 mg

Interventions

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

Cohort 2: Letrozol 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

Cohort 3: Letrozol LEBE 225 mg

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

Cohort 1: Letrozol LEBE 75 mg

Eligibility Criteria

• Age: 18 Years - 75 Years
• Sex: female
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• 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.

You may not qualify if:

• 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.
• Subjects who have history of any significant chronic disease.
• History of cancer within the past 5 years with the exception of non-melanoma skin cancer.
• Subjects who have a history of drug-dependence, and recent history of alcoholism or abuse of alcohol.
• Subjects who have received a drug in research or have participated in other clinical trials within 90 days, prior to dosing.
• Any other unspecified reason that, in the opinion of the investigator (or designee) or sponsor, makes the subject unsuitable for enrolment.

Sponsors & Collaborators

• Rovi Pharmaceuticals Laboratories: lead

Study Sites (1)

Investigational Site number CZ-01

Prague, Czechia

Location

MeSH Terms

Conditions

Breast Neoplasms

Condition Hierarchy (Ancestors)

Neoplasms by Site; Neoplasms; Breast Diseases; Skin Diseases; Skin and Connective Tissue Diseases

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SEQUENTIAL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: March 11, 2024
• First Posted: March 18, 2024
• Study Start: July 26, 2023
• Primary Completion: March 1, 2026
• Study Completion: March 1, 2026
• Last Updated: March 4, 2026

Record last verified: 2026-03

Locations

CZ (1)