Williams Cancer Institute



It has been discussed how the use of dexamethasone for nausea related to chemo needs to be reconsidered since it may negatively affect the response, especially when immunotherapy is involved. Emend, generic name aprepitant is also an option for chemo induced nausea. Unlike dexamethasone, it may be anti-cancer.

Cancer remains a global health challenge, and chemotherapy, despite its limitations, stands as a cornerstone in treatment. This is where aprepitant comes into play. This NK-1R antagonist positions itself as an antitumoral therapeutic strategy, highlighting its ability to induce apoptosis in cancer cells.

NK-1R Antagonists: Aprepitant as a Therapeutic Innovation

Walking the path of NK-1R antagonists, aprepitant emerges as a key player. Both peptidic and non-peptidic antagonists have been explored, but it is the latter, with its high selectivity and efficacy, that takes center stage. Besides combating nausea, this drug has proven to be antiemetic, antipruritic, antiviral, and antitumoral.

Challenges and Advances in Aprepitant Utilization

Not without challenges, peptidic antagonists have revealed limitations, while non-peptidic ones, led by aprepitant, showcase impressive versatility. Its ability to cross the blood-brain barrier and address various conditions, from anxiety to inflammation, underscores its potential.

Repositioning of Aprepitant: A New Approach in Oncology

Aprepitant, approved for clinical use in 2003, goes beyond being merely an antiemetic. It is recognized as a promising antitumoral agent, with in vitro and in vivo studies supporting its ability to induce apoptosis in different cancer cell lines. The exploration of innovative formulations seeks to optimize its bioavailability and efficacy.

SP/NK-1R System: A Potential Biomarker for Cancer

The SP/NK-1R system emerges as a possible biomarker in cancer. Elevated levels are associated with advanced stages and worse prognoses. Identifying this pathway as a target opens new doors for more accurate diagnoses and prognoses.

Aprepitant: A Multifaceted Compound Impacting Cancer Biology

Aprepitant goes beyond being a mere antagonist. Its ability to modulate key pathways and its synergistic potential with other compounds reinforce its role in the fight against cancer. The possibility of reconfiguring it to treat recurrent glioblastomas highlights the potential of drug repositioning.

Conclusions: Aprepitant as a Promising Ally in the Fight Against Cancer. Aprepitant stands as a multifaceted compound. From inducing apoptosis to modulating signaling pathways, its impact on cancer biology opens a new chapter in oncology. The reevaluation and repositioning of this drug offer hopes for more effective and safer therapies for patients in their battle against cancer.

Reference: Miguel Muñoz & Rafael Coveñas, 20 September 2020. The Neurokinin-1 Receptor Antagonist Aprepitant: An Intelligent Bullet against Cancer? https://doi.org/10.3390/cancers12092682

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