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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)