Apalutamide: First Global Approval

@article{AlSalama2018ApalutamideFG,
  title={Apalutamide: First Global Approval},
  author={Zaina T. Al-Salama},
  journal={Drugs},
  year={2018},
  volume={78},
  pages={699-705}
}
Apalutamide (ErleadaTM) is a next-generation oral androgen receptor (AR) inhibitor that is being developed by Janssen for the treatment of prostate cancer (PC). It binds directly to the ligand-binding domain of the AR and blocks the effects of androgens. In February 2018, apalutamide received its first global approval in the USA for the treatment of non-metastatic castration-resistant PC (nmCRPC). Apalutamide is undergoing phase III investigation in chemotherapy-naive patients with metastatic… 
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26 Citations

Apalutamide: A novel therapy for non metastatic castration-resistant carcinoma prostate
  • S. Jayasimha
  • Medicine
    Indian journal of urology : IJU : journal of the Urological Society of India
  • 2018
The recently published trial from the SPARTAN group evaluated the role of adding Apalutamide, a pure androgen receptor antagonist to androgen deprivation therapy (ADT) in patients with high risk, non…
Apalutamide for patients with metastatic castration-sensitive prostate cancer in East Asia: a subgroup analysis of the TITAN trial
TLDR
The efficacy and safety of apalutamide in the East Asian subgroup of the TITAN trial are consistent with the global results.
Comparison of the effect of the antiandrogen apalutamide (ARN-509) versus bicalutamide on the androgen receptor pathway in prostate cancer cell lines
TLDR
Evidence has been reported that ARN is more potent than bicalutamide in blocking the AR pathway in normoxia and in hypoxia, and this reflects a more robust, dose-dependent, repressive effect on cell proliferation.
Therapy of Advanced Prostate Cancer: Targeting the Androgen Receptor Axis in Earlier Lines of Treatment
TLDR
The key clinical trials that led to FDA approval of ARAT in the mHSPC and nmCRPC settings are summarized and potential limitations, future directions, and treatment-algorithms when selecting patients for early therapy are highlighted.
Timing of androgen deprivation monotherapy and combined treatments in castration-sensitive and castration-resistant prostate cancer: a narrative review
TLDR
Early standard ADT can reduce symptoms of disease progression and may extend progression-free and overall survival, and is increasingly combined with new antihormonal drugs in castration-sensitive metastatic prostate cancer to gain additional survival and quality of life benefits.
Previous, Current, and Future Pharmacotherapy and Diagnosis of Prostate Cancer—A Comprehensive Review
TLDR
Possible combinations of new vaccines or immune checkpoint blockers with enzalutamide, abiraterone, radium-223, or docetaxel are the subject of ongoing rivalry regarding optimal therapy of prostate cancer.
Therapies Targeted to Androgen Receptor Signaling Axis in Prostate Cancer: Progress, Challenges, and Hope
TLDR
The importance of androgen signaling in prostate cancer biology and advances made over the years to effectively target this signaling pathway are described and the potential of this knowledge for translation into future therapies for prostate cancer is discussed.
Gonadotropin-Releasing Hormone Receptors in Prostate Cancer: Molecular Aspects and Biological Functions
TLDR
GnRH-based bioconjugates (cytotoxic drugs covalently linked to a Gn RH-based decapeptide) have been recently developed, and the rationale of this treatment is that the GnRH peptide selectively binds to its receptors, delivering the cytotoxic drug to CRPC cells while sparing nontumor cells.
An update of new small-molecule anticancer drugs approved from 2015 to 2020.
Small-Molecule Anti-Cancer Drugs From 2016 to 2020: Synthesis and Clinical Application
TLDR
This paper summarizes the targets and modes of action of the approved anti-tumor drugs while systematically discussing their synthetic routes for medicinal chemistry or industrial use, which will benefit next-generation drug discovery.
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