Analysis of the targets of new drugs on the global market in 2020
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Analysis of the targets of new drugs on the global market in 2020
Analysis of the targets of new drugs on the global market in 2020. In 2020, a total of 61 innovative drugs have been approved in the United States, the European Union and Japan, some of which have innovative biomolecular target mechanisms.
| Drug | Attributes | Target mechanism | Target classification | Indications | Approval |
| Bempedoic acid | Small molecule inhibitor | ATP-citrate synthase (ACLY) | Enzyme | Hypercholesterolemia | FDA,EMA |
| Tazemetostat | Small molecule inhibitor | Histone Lysine N-Methyltransferase EZH2 (EZH2) | Enzyme | Epithelioid sarcoma and follicular lymphoma | FDA |
| Lonafarnib | Small molecule inhibitor | Farnesyltransferase (FPT) | Enzyme | Hutchinson – Guildford Progeria Syndrome (HGPS) and Progeria-like Laminopathy | FDA |
| Cedazuridine | Small molecule inhibitor | Cytidine Dehydrogenase (CDA) | Enzyme | Myelodysplastic syndrome | FDA |
| Remdesivir | Small molecule inhibitor | SARS-CoV-2RNA-dependent RNA polymerase (RdRp) | Enzyme | COVID-19 | FDA, EMA, PMDA |
| Bulevirtide | Peptides | Sodium/bile acid transporter (SLC10A1) | Transporter | Chronic hepatitis D virus infection | EMA |
| Ansuvimab ； atoltivimab ， odesivimab ， maftivimab | Monoclonal antibody | Ebola virus glycoprotein (EBOV GP) | Viral glycoprotein | Ebola virus infection | FDA |
| Belantamab mafodotin | Antibody Drugs (ADC) | TNF receptor superfamily member 17 (TNFRSF17, BCMA) | Tumor-associated antigen | Multiple myeloma | FDA,EMA |
| Sacituzumab govitecan | ADC | Tumor-related calcium signal sensor 2 (TACSTD2, TROP2) | Tumor-associated antigen | Triple negative breast cancer | FDA |
| Lumasiran | siRNA | Oxyacid oxidase 1 (HAO1) | RNA | Type I hyperoxaluria | FDA,EMA |
| Borofalan(10B) | 10B-labeled BPA for Boron Neutron Capture Therapy (BNCT) | Y+L amino acid transporter 1 (SLC7A7) | Transporter | Head and neck cancer | PMDA |
| Ga 68 PSMA-11 | Imaging agent | Prostate specific antigen (KLK3) | Tumor-associated antigen | Prostate cancer diagnosis | FDA |
| Flortaucipir F 18 | Imaging agent | Microtubule-associated protein tau (MAPT) | Structural skeleton | Alzheimer’s disease (AD) diagnosis | drug |
Based on the analysis of literature, here are some of the important drugs and their targets.
Among the targets of the above-mentioned drugs, five (Bempedoic acid, Tazemetostat, Lonafarnib, Cedazuridine, Remdesivir) are enzymes that are inhibited by small molecule drugs, and four are human-derived proteins.
It is worth noting that the target protein of Remdesivir is SARS-CoV-2 RNA-dependent RNA polymerase, which is the first drug approved by the entire FDA to treat COVID-19.
Another viral target is the Ebola virus glycoprotein. For this protein, four innovative monoclonal antibodies (Ansuvimab, atoltivimab, odesivimab, maftivimab) have been approved, three of which are used as a combination therapy, and one can be a single agent.
In addition to small molecules and monoclonal antibodies, three other drug targets are based on therapeutic platforms. Two of them are antibody-drug conjugates (Belantamab mafodotin, Sacituzumab govitecan), which recognize the tumor-specific targets BCMA and TROP2, respectively, to selectively deliver cytotoxic components to tumor cells-the microtubule blocker monomethyl Austenite Bactericin F and topoisomerase I inhibitor SN-38.
The third drug lumasiran is the third approved small interfering RNA therapy, which treats rare disease type 1 hyperoxaluria by reducing the mRNA of oxyacid oxidase 1.
From the perspective of the therapeutic field, the above-mentioned seven innovative target mechanism drugs are used to treat rare diseases, including two family genetic diseases, two viral infections and three cancers.
In addition, there is a boron delivery agent (Borofalan) for tumor boron neutron capture therapy and two (Ga 68 PSMA-11, Flortaucipir F 18) for the diagnosis of prostate cancer and Alzheimer’s disease. The image agent is approved.
(source:internet, reference only)
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