anti-androgen

Bicalutamide (ICI-176334), a synthetic, nonsteroidal antiandrogen, competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens.

Nilutamide (RU23908), an antineoplastic hormonal agent, is mainly used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors, but not for estrogen, progestogen, or glucocorticoid receptors. Therefore, Nilutamide can block the action of androgens of testicular and adrenal origin that stimulate the growth of malignant and normal prostatic tissue. Prostate Y is mainly androgen-dependent and can be treat with chemical castration or surgical. So far, antiandrogen monotherapy has not consistently been certified to be equivalent to castration.

2,2,5,7,8-Pentamethyl-6-Chromanol (PMC) is the antioxidant component of vitamin E (α-tocopherol) and exhibits significant androgen receptor (AR) signaling modulation and anti-cancer activity against prostate cancer cell lines.

RU 58841 (PSK-3841) is a specific androgen receptor antagonist with significant effects on hair regrowth.

SK33 is a potent and tissue selective anti-androgen agent. SK33 reduces androgen receptor (AR) transcriptional activity.

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy.

LX1, an anti-prostate cancer compound, specifically targets the androgen receptor (AR), AR variants, and the steroidogenic enzyme AKR1C3. It inhibits AKR1C3's enzymatic function, decreases the conversion of androstenedione to testosterone, and reduces the expression of both AR and AR-V7, subsequently downregulating their target genes. Additionally, LX1 is effective in overcoming tumor cell resistance to Enzalutamide, and when combined with Enzalutamide, it further suppresses tumor growth.

Gridegalutamide exhibits anti-androgen and anti-tumor activities.

Pentomone (LY-113935) is an anti-androgen compound that acts as a prostate growth inhibitor.

Cyproterone, an anti-androgen, is used in combination with estrogen for the therapy of hirsutism and severe acne in females and as a palliative in prostatic carcinoma.

Lupeol (Monogynol B) is a novel androgen receptor inhibitor with anti-inflammatory and antioxidant activity.

Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α-glucosidase, PTP1B, and RLAR. Vicenin 2 has hepatoprotective, anti-cancer, antioxidant and anti-inflammatory activities, and DTL co-administration is more effective than either of the single agents in androgen-independent prostate cancer. Vicenin 2 might be a useful lead for the development of multiple target-oriented therapeutic modalities for the treatment of diabetes and diabetes-associated complications. Vicenin 2 could act as a UV light barrier to protect the plants.

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.Phase 1.

EPI-001 is an androgen receptor N-terminal domain antagonist with IC50 of ～6 μM and a selective PPAR-gamma modulator.

A-849519 is a reversible inhibitor of MetAP2 that has demonstrated anti-angiogenesis and anticancer activity in a number of in vitro and in vivo models. In this study, we evaluated the anticancer activity of A-849519 in a modified Dunning model of androgen-independent prostate cancer and compared its efficacy with TNP-470, an established MetAP2 inhibitor.

RLA-4842, an iron activator with anti-androgen properties, exhibits anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

RLA-5331 is an anti-androgen compound with iron-activating properties, demonstrating anti-proliferative effects on the metastatic castration-resistant prostate cancer (mCRPC) cell line [1].

Galloylalbiflorin (6′-O-Galloylalbiflorin), an androgen receptor (AR) antagonist with an IC50 value of 53.3 μM, is a compound isolated from the roots of Paeonia lactiflora. It exhibits anti-androgen activity [1].

N-Nitrosodicyclohexylamine (NDCHA), an N-nitrosocompound, exhibits anti-androgenic activity by competitively binding to the androgen receptor (AR) in opposition to 5α-dihydrotestosterone and reducing AR protein levels [1].

Isosilybin B is a flavonolignan extracted from silymarin that exhibits anti-prostate cancer (PCA) activity, inhibits cancer cell proliferation, and contributes to G1-phase blockade and apoptosis.Isosilybin B induces degradation of the androgen receptor.

(E)-6-O-(p-coumaroyl)scandoside methyl ester shows moderate anti-proliferation effect on PC3 human androgen-independent prostate cancer cells.

Ailanthone (AIL) is a natural compound derived from the tree Ailanthus altissima and has anti-hepatocellular carcinoma (HCC) properties. It can induce G0/G1 phase cell cycle arrest by downregulating the expression of cyclins and CDKs, while upregulating the expression of p21 and p27. Additionally, Ailanthone is a potent androgen receptor (AR) inhibitor, capable of inhibiting both the full-length androgen receptor (IC50: 69 nM) and constitutively active splice variants (IC50: 309 nM).