<p>G protein-coupled receptors (GPCRs) are often stated to constitute the target of 30% (or even more) of all approved drugs. This number, probably first mentioned in (<a href="https://pubmed.ncbi.nlm.nih.gov/12209152/">https://pubmed.ncbi.nlm.nih.gov/12209152/</a>) and later has been&#xa0;often cited by many other studies and in some studies even taken for granted, but is this true? In this study, the number of approved drugs acting on GPCRs was analyzed in relation to the total number of approved drugs in Germany. Newly approved drugs in the years 1987–2023 were analyzed. Of the newly approved drugs in Germany in this period, 209 out of 1110 drugs (19%) act primarily on GPCRs. The most common drug target during this period were enzymes (mostly inhibitors), followed by receptor agonists and antagonists. Among all receptor classes, GPCRs are the most common drug target. In recent years, there has been an increase in antibody approvals, making them the fourth most common drug class in the time from 1987–2023. For the years 1999/2000, 2002 and 2023, all drugs listed in the WHO Model List of Essential Medicines were examined regarding targeting GPCRs. In none of the years do more than 15% of the drugs act on GPCRs. 63 of 293 drugs (22%) of&#xa0;the drug list (version 1.0) and 103 of 464 (22%) of&#xa0;version 2.0 of the Institut für Medizinische und Pharmazeutische Prüfungsfragen (Institute for Medical and Pharmaceutical Review Questions) in Germany were identified as GPCR drugs. All drugs of&#xa0;the Rote Liste (Red List) from 2002 and 2023 were examined regarding targeting GPCRs, resulting in a share of 20%. The frequently cited 30% in the drug studies conducted to date mostly refers to FDA-approved drugs. Therefore, the proportion of GPCR-mediated FDA approved drugs does not match the newly approved drugs in Germany or other analyzed sources. This study sends a note of caution to researchers when using data without further specification or precise context in the literature. Such numbers should be analyzed critically and not taken for granted in every situation.</p>

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Do GPCRs constitute the target of 30% of newly approved drugs in Germany?

  • Sophia Schröer,
  • Roland Seifert

摘要

G protein-coupled receptors (GPCRs) are often stated to constitute the target of 30% (or even more) of all approved drugs. This number, probably first mentioned in (https://pubmed.ncbi.nlm.nih.gov/12209152/) and later has been often cited by many other studies and in some studies even taken for granted, but is this true? In this study, the number of approved drugs acting on GPCRs was analyzed in relation to the total number of approved drugs in Germany. Newly approved drugs in the years 1987–2023 were analyzed. Of the newly approved drugs in Germany in this period, 209 out of 1110 drugs (19%) act primarily on GPCRs. The most common drug target during this period were enzymes (mostly inhibitors), followed by receptor agonists and antagonists. Among all receptor classes, GPCRs are the most common drug target. In recent years, there has been an increase in antibody approvals, making them the fourth most common drug class in the time from 1987–2023. For the years 1999/2000, 2002 and 2023, all drugs listed in the WHO Model List of Essential Medicines were examined regarding targeting GPCRs. In none of the years do more than 15% of the drugs act on GPCRs. 63 of 293 drugs (22%) of the drug list (version 1.0) and 103 of 464 (22%) of version 2.0 of the Institut für Medizinische und Pharmazeutische Prüfungsfragen (Institute for Medical and Pharmaceutical Review Questions) in Germany were identified as GPCR drugs. All drugs of the Rote Liste (Red List) from 2002 and 2023 were examined regarding targeting GPCRs, resulting in a share of 20%. The frequently cited 30% in the drug studies conducted to date mostly refers to FDA-approved drugs. Therefore, the proportion of GPCR-mediated FDA approved drugs does not match the newly approved drugs in Germany or other analyzed sources. This study sends a note of caution to researchers when using data without further specification or precise context in the literature. Such numbers should be analyzed critically and not taken for granted in every situation.