&lt;p&gt;Clinical Evaluation of Everolimus in the Treatment of Neuroendocrine Tumors of the Lung: Patient Selection and Special Considerations. A Systematic and Critical Review of the Literature&lt;/p&gt;

Peri, Marta; Fazio, Nicola

doi:10.2147/lctt.s249928

Cited by 5 publications

(3 citation statements)

References 76 publications

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“…[42][43][44] Given the heterogeneity of NENs, their management and treatment is complex. 45 Recently developed treatments include somatostatin analogs, everolimus, 46 temozolomide plus capecitabine, sunitinib, and peptide receptor radionuclide therapy. 47 Despite an increase in treatment options for patients with NENs, an unmet medical need remains for additional novel therapies that provide optimal disease management.…”

Section: Discussionmentioning

confidence: 99%

Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies

Hollebecque

Salvagni

Plummer

et al. 2022

Cancer

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Background CC‐90011 is an oral, potent, selective, reversible inhibitor of lysine‐specific demethylase 1 (LSD1) that was well tolerated, with encouraging activity in patients who had advanced solid tumors or relapsed/refractory marginal zone lymphoma. The authors present long‐term safety and efficacy and novel pharmacodynamic and pharmacokinetic data from the first‐in‐human study of CC‐90011. Methods CC‐90011‐ST‐001 (http://clincaltrials.gov identifier NCT02875223; Eudract number 2015–005243‐13) is a phase 1, multicenter study in which patients received CC‐90011 once per week in 28‐day cycles. The objectives were to determine the safety, maximum tolerated dose, and/or recommended phase 2 dose (primary) and to evaluate preliminary efficacy and pharmacokinetics (secondary). Results Sixty‐nine patients were enrolled, including 50 in the dose‐escalation arm and 19 in the dose‐expansion arm. Thrombocytopenia was the most common treatment‐related adverse event and was successfully managed with dose modifications. Clinical activity with prolonged, durable responses were observed, particularly in patients who had neuroendocrine neoplasms. In the dose‐escalation arm, one patient with relapsed/refractory marginal zone lymphoma achieved a complete response (ongoing in cycle 58). In the dose‐expansion arm, three patients with neuroendocrine neoplasms had stable disease after nine or more cycles, including one patient who was in cycle 46 of ongoing treatment. CC‐90011 decreased levels of secreted neuroendocrine peptides chromogranin A, progastrin‐releasing peptide, and RNA expression of the blood pharmacodynamic marker monocyte‐to‐macrophage differentiation–associated. Conclusions The safety profile of CC‐90011 suggested that its reversible mechanism of action may provide an advantage over other irreversible LSD1 inhibitors. The favorable tolerability profile, clinical activity, durable responses, and once‐per‐week dosing support further exploration of CC‐90011 as monotherapy and in combination with other treatments for patients with advanced solid tumors and other malignancies.

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Section: Discussionmentioning

confidence: 99%

Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies

Hollebecque

Salvagni

Plummer

et al. 2022

Cancer

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“…AC presents metastatic spread in up to one half of cases and has a median time to recurrence of 1.8 years. As for advanced lung NET, median survival from diagnosis is about 6-7 years [59]. Concerning treatment, it worth considering a different approach based on the histological group and patients tailored.…”

Section: Lung Neuroendocrine Neoplasmsmentioning

confidence: 99%

"Present and future of immunotherapy in Neuroendocrine Tumors"

Albertelli

Dotto

Nista

et al. 2021

Rev Endocr Metab Disord

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Immunotherapy, so promising in many neoplasms, still does not have a precise role in the treatment of neuroendocrine neoplasms (NENs). In this article, we provide an overview on the current knowledge about immunotherapy with immune checkpoint inhibitors (ICIs) applied to NENs, evaluating future perspectives in this setting of tumors.Evidence so far available for ICIs in gastroenteropancreatic (GEP)-NENs is definitively not as robust as for other tumors such as Small Cell Lung Cancer or Merkel Cell Carcinoma. In fact, with regard to the well-differentiated forms of NENs (NETs), the results obtained nowadays have been disappointing. However, the near future, might reserve interesting results for ICIs in GEP-NEN from a total of nine different ICI drugs, used throughout 19 randomised controlled trials. Such numbers highlight the growing attention gathering around NENs and ICIs, in response to the need of stronger evidences supporting such therapy.For the future, the most important aspect will be to study strategies that can make NETs more susceptible to response to ICI and, thus, enhance the effectiveness of these treatments. Therefore, the combination of conventional therapy, target therapy and immunotherapy deserve attention and warrant to be explored. A sequential chemotherapy, possibly inducing an increase in tumor mutational burden and tested before immunotherapy, could be a hypothesis deserving more consideration. A radiation treatment that increases tumor-infiltrating lymphocytes, could be another approach to explore before ICIs in NENs. Equally essential will be the identification of biomarkers useful for selecting patients potentially responsive to this type of treatment.

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“…On 20 July 2012, the U.S. FDA approved Everolimus for the treatment of post-menopausal women with advanced HR+/HER2− breast cancer. It is worth mentioning that Everolimus has been approved also for tuberous sclerosis complexassociated partial-onset seizures (in 2018), progressive, nonfunctional gastrointestinal and lung neuroendocrine tumors (in 2016), and advanced pancreatic neuroendocrine tumors (in 2011), as well as being the first approved pediatric-specific dosage form for the management of a rare pediatric brain tumor called subependymal giant cell astrocytoma [29][30][31].…”

Section: Everolimusmentioning

confidence: 99%

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

Elkaeed

Salam²,

Sabt³

et al. 2021

Molecules

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Among all cancer types, breast cancer (BC) still stands as one of the most serious diseases responsible for a large number of cancer-associated deaths among women worldwide, and diagnosed cases are increasing year by year worldwide. For a very long time, hormonal therapy, surgery, chemotherapy, and radiotherapy were used for breast cancer treatment. However, these treatment approaches are becoming progressively futile because of multidrug resistance and serious side effects. Consequently, there is a pressing demand to develop more efficient and safer agents that can fight breast cancer belligerence and inhibit cancer cell proliferation, invasion and metastasis. Currently, there is an avalanche of newly designed and synthesized molecular entities targeting multiple types of breast cancer. This review highlights several important synthesized compounds with promising anti-BC activity that are categorized according to their chemical structures.

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<p>Clinical Evaluation of Everolimus in the Treatment of Neuroendocrine Tumors of the Lung: Patient Selection and Special Considerations. A Systematic and Critical Review of the Literature</p>

Cited by 5 publications

References 76 publications

Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies

Clinical activity of CC‐90011, an oral, potent, and reversible LSD1 inhibitor, in advanced malignancies

"Present and future of immunotherapy in Neuroendocrine Tumors"

Recent Advancements in the Development of Anti-Breast Cancer Synthetic Small Molecules

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