A drug–drug interaction study of everolimus (an mTOR inhibitor) and JI-101, an orally active inhibitor of VEGF 2, PDGF, and EphB4 receptors, in patients with advanced urologic tumors.

Agarwal, Neeraj; Sahu, Mukesh; Abhyankar, Dhiraj; Werner, Theresa L.; Benjamin, Biju; Srinivas, N. R.; Sharma, Somesh

doi:10.1200/jco.2011.29.15_suppl.e15077

Cited by 2 publications

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“…Considering the ability to inhibit both angiogenesis and proliferation, combination therapies with mTOR inhibitors, such as everolimus, and PI3K inhibitors are considered [18,159,163]. In a small clinical study, no serious adverse side effects were observed when assessing the combination therapy of JI-101 and everolimus [163]. In another study, the most frequent side-effect was hypertension, which is seen in a variety of angiogenesis inhibitors [18].…”

Section: Ji-101 and Xl647mentioning

confidence: 99%

“…In another study, the most frequent side-effect was hypertension, which is seen in a variety of angiogenesis inhibitors [18]. Both studies warrant further clinical evaluation [18,163]. Currently no clinical trials are recruiting, but, based on the results, future studies on combination treatments with drugs such as everolimus show promise.…”

Section: Ji-101 and Xl647mentioning

confidence: 99%

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The role of Eph receptors in cancer and how to target them: novel approaches in cancer treatment

Buckens

Hassouni

Giovannetti

et al. 2020

Expert Opinion on Investigational Drugs

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Introduction: Erythropoietin-producing human hepatocellular (Eph) receptors are among the largest family of tyrosine kinases that are divided into two classes: EphA and EphB receptors. Over the past two decades, their role in cancer has become more evident. Areas covered: There is a need for new anticancer treatments and more insight in the emerging role of Eph receptors in cancer. Molecular mechanisms underlying the pro-tumorigenic effects of Eph receptors could be exploited for future therapeutic strategies. This review describes the variability in expression levels and different effects on oncogenic and tumor suppressive downstream signaling of Eph receptors in various cancer types, and the small molecules, antibodies and peptides that target these receptors. Expert opinion: The complexity of Eph signaling is a challenge for the definition of clear targets for cancer treatment. Nevertheless, numerous drugs that target EphA2 and EphB4 are currently in clinical trials. However, some Eph targeted drugs also inhibit other tyrosine kinases, so it is unclear to what extent the targeting of Eph receptors contributes to their efficacy. Future research is warranted for an improved understanding of the full network in which Eph receptors function. This will be critical for the improvement of the anticancer effects of drugs that target the Eph receptors.

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Section: Ji-101 and Xl647mentioning

confidence: 99%

Section: Ji-101 and Xl647mentioning

confidence: 99%

The role of Eph receptors in cancer and how to target them: novel approaches in cancer treatment

Buckens

Hassouni

Giovannetti

et al. 2020

Expert Opinion on Investigational Drugs

View full text Add to dashboard Cite

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Novel targets for VEGF-independent anti-angiogenic drugs

Petrillo

Scambia

Ferrandina

2012

Expert Opinion on Investigational Drugs

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Besides the successful development of drugs providing a specific VEGF blockade, novel agents targeting alternative angiogenesis-related pathways are being tested. Although it seems that the potential clinical usefulness of these novel compounds have been not yet fully investigated, sunitinib, sorafenib, pazopanib and other multikinase inhibitors have certainly displayed encouraging results. A more in-depth clarification of anti-angiogenic agents is still needed, in order to design the best clinical setting and schedule for target-based agents and possibly anticipate potential tools to overcome the emerging issue of anti-angiogenic drug resistance.

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A drug–drug interaction study of everolimus (an mTOR inhibitor) and JI-101, an orally active inhibitor of VEGF 2, PDGF, and EphB4 receptors, in patients with advanced urologic tumors.

Cited by 2 publications

References 0 publications

The role of Eph receptors in cancer and how to target them: novel approaches in cancer treatment

The role of Eph receptors in cancer and how to target them: novel approaches in cancer treatment

Novel targets for VEGF-independent anti-angiogenic drugs

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