Phase 1, First-in-Human Study of RAD140 in Postmenopausal Women With Breast Cancer

This is a first in humans study that is designed to evaluate the clinical safety profile,
tolerability, and pharmacokinetic (PK) characteristics of RAD140 in hormone receptor positive
breast cancer.

Key Inclusion Criteria:

- Progressive metastatic or locally advanced or metastatic breast cancer.

- Clinically confirmed as postmenopausal.

- Eastern Cooperative Oncology Group (ECOG) score of 0 to 1 at screening.

Key Exclusion Criteria:

- HER2 positive patients by local laboratory testing.

- Triple negative breast cancer.

- Any chemotherapy within the 28 days prior to the first dose of study drug.

- Any non-chemotherapy anti-cancer drug less than 5 half-lives (30 days for biologics)
or less than 14 days for small molecule therapeutics, or if half-life is not known.

- Tamoxifen and aromatase inhibitors within 14 days prior to the first dose of study
drug.

- Fulvestrant within 30 days prior to first dose of study drug.

- Any investigational drug therapy within 5 half-lives of the previous investigational
study drug or 30 days, whichever is shorter.

- Radiation therapy for breast cancer within 2 weeks of dosing and planning to have
radiation therapy during participation in this study.

- Known history of human immunodeficiency virus infection (HIV) or hepatitis C or active
hepatitis B infection, unless the patient was diagnosed >10 years prior to enrollment
and no evidence of active liver disease.

- Currently taking testosterone, methyltestosterone, oxandrolone (Oxandrin),
oxymetholone, danazol, fluoxymesterone (Halotestin), or testosterone-like agents.

- Untreated or uncontrolled brain metastasis.

- Diagnosed with or treated for cancer within the previous 2 years, other than breast
cancer or non-melanoma carcinoma of the skin.

- Pregnant and nursing females.