New pharmaceuticals approved by FDA in 2020: Small‐molecule drugs derived from amino acids and related compounds

Liu, Aiyao; Han, Jianlin; Nakano, Arina; Konno, Hiroyuki; Moriwaki, Hiroki; Abe, Hidenori; Izawa, Kunisuke; Soloshonok, Vadim A.

doi:10.1002/chir.23376

Cited by 27 publications

(22 citation statements)

References 150 publications

(250 reference statements)

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“…In the recent years, multiple 68 Ga-and 18 F-labelled PSMA-targeting radiotracers have been introduced and recommended in several guidelines (10)(11)(12). Furthermore, 68 Ga-PSMA-11 and 18 F-DCFPyL received recent FDA-approval for imaging of BCR (13,14).…”

Section: Psma-pet For Recurrent Pcamentioning

confidence: 99%

Editorial: Exploring the Potential of PSMA-PET Imaging on Personalized Prostate Cancer Treatment

et al. 2022

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Editorial on the Research TopicExploring the Potential of PSMA-PET Imaging on Personalized Prostate Cancer Treatment INTRODUCTIONProstate cancer (PCa) is the second most frequent cancer diagnosis made in men worldwide (1). Accurate and reliable diagnostic medical imaging is a frequent prerequisite for personalized treatment approaches in patients with PCa by enabling, in part, (i) understanding extent of disease, (ii) accurate segmentation of PCa lesions and, (iii) non-invasive tumor characterization, for example, using radiomics or artificial intelligence tools (2).Prostate Specific Membrane Antigen (PSMA) has been found to be selectively overexpressed in PCa cells (3) and can be traced by radio-labelled peptide ligands in positron emission tomography (PSMA-PET). First studies suggested excellent diagnostic accuracy and a major impact on therapeutic approaches for PSMA-PET in newly diagnosed (4), recurrent (5) or metastatic PCa patients (4). The goal of this Research Topic was to concentrate scientific contributions on the growing evidence of integrating PSMA-PET imaging in personalized PCa treatment concepts.The Research Topic accepted 15 articles including a total of 126 authors, demonstrating the growing interest in the field of PSMA-PET imaging. The manuscripts of the Research Topic can be divided into the following topics.

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Section: Psma-pet For Recurrent Pcamentioning

confidence: 99%

Editorial: Exploring the Potential of PSMA-PET Imaging on Personalized Prostate Cancer Treatment

et al. 2022

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“…Tailor-made amino acids [1] play an indispensable role in the development of modern pharmaceuticals and drug formulations [2][3][4][5][6]. Thus, over 20% of newly approved smallmolecule drugs contain structural fragments of AAs [7][8][9]. In particular, γ-aminobutyricacid (GABA) derivatives bearing β-alkyl or β-aryl substituents, which include baclofen [10], phenibut [11][12][13], tolibut [14], and pregabalin [15][16][17], are recognized as an essential class of marketed pharmaceuticals for the treatment of neurological diseases (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives

et al. 2022

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γ-Aminobutyric acid (GABA) represents one of the most prolific structural units widely used in the design of modern pharmaceuticals. For example, β-substituted GABA derivatives are found in numerous neurological drugs, such as baclofen, phenibut, tolibut, pregabalin, phenylpiracetam, brivaracetam, and rolipram, to mention just a few. In this review, we critically discuss the literature data reported on the preparation of substituted GABA derivatives using the Michael addition reaction as a key synthetic transformation. Special attention is paid to asymmetric methods featuring synthetically useful stereochemical outcomes and operational simplicity.

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“…The synthetic amino acid anti-1-amino-3-[ 18 F]-flurocyclobutane-1-carboxylic acid (namely, 18 F-FACBC, 18 F-fluciclovine, Axumin ® ) is an L-leucine analogue showing high tumor accumulation by addressing amino acid transports, which are up-regulated in PC [ 7 ]. On the other hand, PET/CT with ligands binding to Prostate Specific Membrane Antigen (PSMA), overexpressed by PC and only minimally detectable in normal prostate tissue, has recently been introduced with overwhelming results in clinical practice, and two PSMA-targeted radiopharmaceuticals have recently been FDA approved [ 8 , 9 ]. However, some PSMA ligands (e.g., 68 Ga-PSMA-11) show a meaningful accumulation in bladder; thus, the identification of loco-regional relapse might deserve particular attention and require dedicated protocols [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Detection Rate and Clinical Impact of PET/CT with 18F-FACBC in Patients with Biochemical Recurrence of Prostate Cancer: A Retrospective Bicentric Study

et al. 2022

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Our aim was to assess the detection rate (DR) of positron emission computed tomography (PET/CT) with anti-1-amino-3-[18F]-flurocyclobutane-1-carboxylic acid (18F-FACBC) in patients with biochemical recurrence (BCR) from prostate cancer (PC). As a secondary endpoint, we evaluated 18F-FACBC PET/CT’s impact on patients management. Clinical records of 81 patients submitted to 18F-FACBC PET/CT due to PC BCR in two Italian Nuclear Medicine Units were retrospectively assessed. DR was gauged in the whole cohort and stratifying patients by discrete intervals of PSA levels. PET/CT’s impact on clinical management was scored as (1) major if it entailed an intermodality change (e.g., from systemic to loco-regional therapy); (2) minor if it led to an intramodality change (e.g., modified radiotherapy field). PET/CT’s DR resulted in 76.9% in the whole cohort, with a positive predictive value of 96.7%. Stratified by PSA quartile intervals, PET/CT’s DR was 66.7%, 71.4%, 78.9% and 90% for PSA 0.2–0.57 ng/mL, 0.58–0.99 ng/mL, 1–1.5 ng/mL and >1.5 ng/mL without significant difference among groups (p = 0.81). The most common sites of relapse were prostate bed and pelvic lymph nodes (59.3%). PET/CT impacted on clinical management in 33/81 cases (40.7%), leading to a major change in 30 subjects (90.9%). 18F-FACBC PET/CT localized recurrence in patients with BCR, with meaningful DR also at low PSA levels and significantly impacted on clinical management.

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New pharmaceuticals approved by FDA in 2020: Small‐molecule drugs derived from amino acids and related compounds

Cited by 27 publications

References 150 publications

Editorial: Exploring the Potential of PSMA-PET Imaging on Personalized Prostate Cancer Treatment

Editorial: Exploring the Potential of PSMA-PET Imaging on Personalized Prostate Cancer Treatment

Asymmetric Michael Addition in Synthesis of β-Substituted GABA Derivatives

Detection Rate and Clinical Impact of PET/CT with 18F-FACBC in Patients with Biochemical Recurrence of Prostate Cancer: A Retrospective Bicentric Study

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