Medications for treatment of prostate cancer and mode of action
| Sr.No. | Drug name | SMILES | Mode of action | Reference |
|---|---|---|---|---|
| 1 | Apalutamide | CNC(=O)C1=CC=C(C=C1F)N1C(=S)N(C(=O)C11CCC1)C1=CC(=C(N=C1)C#N)C(F)(F)F | Antagonism of androgen receptor (AR) signaling by direct binding to the ligand-binding domain, inhibiting DNA binding, AR-mediated gene transcription, and AR translocation from cytoplasm to nucleus, thereby reducing AR availability to interact with androgen response elements (AREs). | [50] |
| 2 | Bicalutamide | CC(O)(CS(=O)(=O)C1=CC=C(F)C=C1)C(=O)NC1=CC(=C(C=C1)C#N)C(F)(F)F | Bicalutamide competes with androgen for binding to ARs, thus blocking the stimulatory effect of androgens on prostatic tissue growth. | [51] |
| 3 | Cabazitaxel | [H][C@]12[C@H](OC(=O)C3=CC=CC=C3)[C@]3(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C4=CC=CC=C4)C(C)=C([C@@H](OC)C(=O)[C@]1(C)[C@H](C[C@H]1OC[C@@]21OC(C)=O)OC)C3(C)C | Stabilization of microtubules by binding to the N-terminal amino acids of the β-tubulin subunit, promoting microtubule polymerization, inhibiting disassembly, and ultimately blocking mitotic and interphase cellular functions, thereby is preventing tumor proliferation. | [52] |
| 4 | Darolutamide | C[C@@H](CN1C=CC(=N1)C1=CC=C(C#N)C(Cl)=C1)NC(=O)C1=NNC(=C1)C(C)O | Competitively inhibits androgen binding to AR, blocking AR nuclear translocation and AR-mediated transcription, resulting in decreased PC cell proliferation and tumor size reduction. It binds more tightly to the AR receptor than other AR antagonists and also acts as a progesterone receptor (PR) antagonist, although the clinical relevance is not fully understood. | [53, 54] |
| 5 | Degarelix | CC(C)CC(C(=O)NC(CCCCNC(C)C)C(=O)N1CCCC1C(=O)NC(C)C(=O)N)NC(=O)C(CC2=CC=C(C=C2)NC(=O)N)NC(=O)C(CC3=CC=C(C=C3)NC(=O)C4CC(=O)NC(=O)N4)NC(=O)C(CO)NC(=O)C(CC5=CN=CC=C5)NC(=O)C(CC6=CC=C(C=C6)Cl)NC(=O)C(CC7=CC8=CC=CC=C8C=C7)NC(=O)C | Competitive inhibition of GnRH receptors in the pituitary gland, leading to decreased release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which in turn reduces testosterone release from the testes, slowing the growth and reducing the size of PCs. | [55, 56] |
| 6 | Docetaxel | [H][C@@]1(C[C@@]2(O)[C@@H](OC(=O)C3=CC=CC=C3)[C@]3([H])[C@@]4(CO[C@@H]4C[C@H](O)[C@@]3(C)C(=O)[C@H](O)C(=C1C)C2(C)C)OC(C)=O)OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C1=CC=CC=C1 | Stabilizes microtubules by promoting their assembly and preventing depolymerization, leading to disruption of vital cellular functions, abnormal microtubule formation, and induction of apoptosis by binding to Bcl-2. | [57, 58] |
| 7 | Enzalutamide | CNC(=O)C1=C(F)C=C(C=C1)N1C(=S)N(C(=O)C1(C)C)C1=CC=C(C#N)C(=C1)C(F)(F)F | Competitive inhibition of the AR signaling pathway. | [59] |
SMILES: simplified molecular input line entry system
