The present invention contains the A- nor -5α-androstane compounds as the active ingredient, publish oral administration preparation A- nor -5α-androstane compound. Oral administration formulations of the present invention, the active ingredient has an action to suppress a significant malignant tumor cell growth, drug has low toxicity, the therapeutic effect is better, a new antineoplastic drug with targeting and thus do compounds specifically acts only on the tumor cells, without affecting normal cells. The active ingredient further comprises an anti-prostate hypertrophy activity. High stability of the oral formulation, with excellent dissolution properties convenient administration, use is safe and reliable, there are enormous social and economic benefits.