FDA-Approved Small Molecule Compounds as Drugs for Solid Cancers from Early 2011 to the End of 2021

Abstract

Solid cancers are the most common types of cancers diagnosed globally and comprise a large number of deaths each year. The main challenge currently in drug development for tumors raised from solid organs is to find more selective compounds, which exploit specific molecular targets. In this work, the small molecule drugs registered by the Food and Drug Administration (FDA) for solid cancers treatment between 2011 and 2022 were identified and analyzed by investigating a type of therapy they are used for, as well as their structures and mechanisms of action. On average, 4 new small molecule agents were introduced each year, with a few exceptions, for a total of 62 new drug approvals. A total of 50 of all FDA-approved drugs have also been authorized for use in the European Union by the European Medicines Agency (EMA). Our analysis indicates that many more anticancer molecules show a selective mode of action, i.e., 49 targeted agents, 5 hormone therapies and 3 radiopharmaceuticals, compared to less specific cytostatic action, i.e., 5 chemotherapeutic agents. It should be emphasized that new medications are indicated for use mainly for monotherapy and less for a combination or adjuvant therapies. The comprehensive data presented in this review can serve for further design and development of more specific targeted agents in clinical usage for solid tumors.

Drug Delivery Systems for Localized Cancer Combination Therapy

“…These challenges can hinder the success of clinical trials leaving many targeted inhibitors left in preclinical development. 7 More recently, immunotherapies have shifted the landscape of cancer treatment by recruiting and activating an immune response against tumors. Tumors inherently employ a wide range of immunosuppressive mechanisms to evade a hostdirected attack; however, immunotherapies, such as checkpoint inhibitors, stimulatory factors, and immune cell therapies, can mitigate these defense mechanisms and sequester an immune response against the tumor.…”

“…Also, some targeted inhibitors have shown to have affinity for other proteins and receptors resulting in off-target effects upon systemic exposure. These challenges can hinder the success of clinical trials leaving many targeted inhibitors left in preclinical development …”

Studies on the Complexation of Platinum(II) by Some 4-Nitroisoxazoles and Testing the Cytotoxic Activity of the Resulting Complexes

“…Advances in research on platinum-based anticancer drugs describing a different approach, including non-classical structures, have been announced in numerous publications [ 16 , 17 , 18 , 19 ]. However, despite efforts in this area, no new platinum complex drug has been introduced into anticancer therapy for more than 10 years [ 20 , 21 ]. In our previous studies [ 22 ], we synthesized and characterized a series of cis and trans platinum(II) complexes with the structural formula trans-[PtCl 2 L 2 ] with substituted nitropyrazole ligands.…”

Synthesis, Anticancer Activity and Molecular Docking Studies of Novel N-Mannich Bases of 1,3,4-Oxadiazole Based on 4,6-Dimethylpyridine Scaffold

“…Scientists around the world are working on new methods of fighting cancer, which would allow for increased effectiveness of treatment and minimization of undesirable effects of the therapy. Additionally, an increasingly accurate understanding of the molecular pathogenesis of carcinogenesis allows for the implementation of targeted therapy that focuses only on tumor cells and reduces side effects on healthy tissues [ 6 ]. A very popular molecular target of new structures is a group of receptors with tyrosine kinase activity.…”