Table 2 Epidrugs approved and in clinical trial for cancer treatment, with respective effects and drug category

Azacitidine Vidaza®

High-risk myelodysplastic syndromes

Chronic Myelomonocytic Leukemia

Acute Myeloid Leukemia

Pancreatic, colorectal, prostate, esophageal, breast, non-small cell lung cancer, thyroid, ovarian, nasopharyngeal and bladder cancer, hematological malignancies sarcoma, melanoma, germ cell tumors and renal cell carcinomas

Nucleoside DNMT inhibitor

Decitabine Dacogen®

High-risk myelodysplastic syndromes

Chronic Myelomonocytic Leukemia

Acute Myeloid Leukemia

Ovary, head and neck, colorectal, breast, esophageal, non-small cell lung, prostate, thyroid cancers, B cell lymphoma, glioma and medulloblastoma

Nucleoside DNMT inhibitor

5′-Fluoro-2′-deoxycytidine (FdCyd)

–

Head and neck, lung, urinary bladder, breast cancer and acute myeloid leukemia

Nucleoside DNMT inhibitor

Guadecitabine

–

Kidney, lung, ovarian, prostate, colorectal, gallbladder, pancreatic, urothelial cancer, extrahepatic bile duct adenocarcinoma, biliary type, testicular germ cell tumors, chondrosarcoma, melanoma, acute myeloid leukemia and myelodysplastic syndrome

Nucleoside DNMT inhibitor

RX-3117 (fluorocyclopentenylcytosine)

–

Pancreatic and bladder cancer

Nucleoside DNMT inhibitor

Genistein

–

Breast, prostate, colorectal, lung, pancreatic, bladder, kidney, endometrial cancer and melanoma

Isoflavone non-nucleoside DNMT inhibitor

Curcumin

–

Prostate, colorectal, breast, lung, head and neck and cervical cancer

Natural phenol non-nucleoside DNMT inhibitor

Hydralazine

–

Ovarian, cervical, lung and breast cancer

Repurposed drug non-nucleoside DNMT inhibitor

Belinostat Beleodaq®

Peripheral T-cell Lymphoma

Lung, breast, ovary, hematological malignancies, bladder, liver cancer and chondrosarcoma

Hydroxamic acid pan-HDAC inhibitor

Givinostat

–

Chronic Myeloproliferative Neoplasms Polycythemia Vera

Hydroxamic acid pan-HDAC inhibitor

Panobinostat Farydak®

Multiple Myeloma

Breast, lung, pancreatic, prostate, colorectal, head and neck, esophageal, neuroendocrine, renal, thyroid, brain cancer, hematologic neoplasms and melanoma

Hydroxamic acid pan-HDAC inhibitor

Trichostatin A

–

Hematological malignancies

Hydroxamic acid pan-HDAC inhibitor

Vorinostat Zolinza®

Cutaneous T cell Lymphoma

Breast, ovarian, pancreatic, lung, colorectal, gastric, liver, prostate, renal, bladder brain cancer, melanoma and hematological malignancies

Hydroxamic acid pan-HDAC inhibitor

Entinostat

–

Breast, colorectal, ovarian, neuroendocrine, lung, prostate, renal, pancreatic, endometrial cancer, hematological malignancies and cholangiocarcinoma

Benzamide class I HDAC inhibitor

Romidepsin Istodax®

Cutaneous T-cell lymphoma

Lung, breast, pancreatic, colorectal, thyroid, bladder, ovarian cancer, glioma and hematological malignancies

Benzamide class I HDAC inhibitor

Valproic acid

–

Cervical, brain, lung. breast, pancreatic, prostate, bladder, thyroid, head and neck cancer and hematological malignancies

Short-chain and aromatic fatty acids pan-HDAC inhibitor

Abexinostat

–

Breast cancer, renal cell carcinoma, sarcoma, melanoma and hematologic malignancies

Hydroxamic acid pan-HDAC inhibitor

Tazemetostat Tazverik®

Advanced epithelioid sarcoma

Follicular lymphoma

Prostate, ovarian, endometrial, head and neck cancer, melanoma, hematological malignancies, urothelial carcinoma and malignant mesothelioma

EZH2 inhibitor

Domatinostat

–

Melanoma and Merkel cell carcinoma

Benzamide class I HDAC inhibitor