Breast Cancer Program - (Z)-endoxifen
Clinical Development Pipeline
Our mission is to develop innovative medicines in areas of significant unmet medical need in oncology.
The Breast Cancer Problem
78%
of US breast cancer is ER+
1 in 8
women experience breast cancer
281,000
women diagnosed in US annually
2nd
leading cause of cancer death in American women
(Z)-endoxifen - New, Proprietary SERM
- According to published studies, (Z)-endoxifen is a competitive inhibitor of ERα and represses ERα transcriptional activity
- (Z)-endoxifen is 100-fold more potent in anti-estrogen activity compared to other SERMs(1)
- (Z)-endoxifen binds to and disrupts protein kinase C beta one function (PKCb1, a known oncogenic protein)
- The National Cancer Institute (NCI) and others have studied (Z)-endoxifen and have demonstrated promising results in the treatment of breast cancer as well as for the treatment of other solid tumors
- Treatment with (Z)-endoxifen may avoid off target effects of tamoxifen and remaining metabolites potentially increasing adherence by improving safety profile
Atossa's Proprietary Oral Formulation
- Atossa has a patented (Z)-endoxifen chemical process and composition of matter
- Enhanced stability of (Z)-endoxifen on the shelf
- Atossa also has a patented oral enteric capsule formulation of (Z)-endoxifen
- Enhanced stability following oral administration
- Capsules of 10 mg and 40 mg are being evaluated in neoadjuvant setting
- Atossa’s (Z)-endoxifen has been studied in numerous non-clinical studies and in four completed Phase 1 or 2 studies at doses of 1 mg/day to 4 mg/day with an acceptable safety profile
Phase 2 Study - EVANGELINE
- Open-label, randomized, Phase 2 study in premenopausal women with Grade 1 or 2 ER+/HER2- breast cancer – first patient was enrolled in February 2023
- Subjects are enrolled with the intent of surgical treatment in the involved breast(s) after completing neoadjuvant study treatment
- Expected to enroll approximately 175 patients at up to 25 sites across the United States
- Primary objective is to evaluate the endocrine sensitive disease rate, measured by Ki-67 compared to treatment with current standard of care
- Current SOC includes medication given to block the ovaries from making estrogen, which in premenopausal women is associated with significant morbidity and inadequate compliance, which compromises efficacy and increases the risk of mortality
Karisma Endoxifen Trial
- Being conducted in Stockholm by South General Hospital – Principal investigator is Per Hall, M.D., Ph.D., Department of Medical Epidemiology and Biostatistics at Karolinska Institute and South General Hospital.
- Primary objective – Pharmacodynamics study to determine the dose-response relationship of daily endoxifen on Mammographic Breast Density (MBD) Reduction.
- Randomized, double-blinded and placebo-controlled.
- 240 pre-menopausal women with measurable MBD dosed for six months.
- Full enrollment occurred in November 2023 with data expected in the second half of 2024.
Phase 2 Study - I-Spy 2
- Ground-breaking platform trial for neoadjuvant treatment of locally advanced breast cancer
- (Z)-endoxifen is being evaluated in the Endocrine Optimization Pilot Protocol targeting patients with newly diagnosed ER+ invasive breast cancer for whom chemotherapy is expected to provide little or no benefit
- These patients have substantial risk for recurrence
- Approximately 20 patients will be treated with (Z)-endoxifen for up to 24 weeks prior to surgery
- Enrolling patients at all 41 I-Spy sites across the United States
