Synonyms: KPT-8602 | KPT8602
Compound class:
Synthetic organic
Comment: Eltanexor (KPT-8602) is a second-generation, orally bioavailable, selective inhibitor of the nuclear export protein XPO1, that works in the same way as its first-in-class relation selinexor. In comparison to selinexor, eltanexor exhibits much lower brain penetration, and this appears to reduce the central nervous system-mediated side effects of anorexia and weight loss detected with selinexor therapy [1]. Eltanexor is being investigated for therapeutic antineoplastic potential [1-3].
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References |
1. Etchin J, Berezovskaya A, Conway AS, Galinsky IA, Stone RM, Baloglu E, Senapedis W, Landesman Y, Kauffman M, Shacham S et al.. (2017)
KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells. Leukemia, 31 (1): 143-150. [PMID:27211268] |
2. Hing ZA, Fung HY, Ranganathan P, Mitchell S, El-Gamal D, Woyach JA, Williams K, Goettl VM, Smith J, Yu X et al.. (2016)
Next-generation XPO1 inhibitor shows improved efficacy and in vivo tolerability in hematological malignancies. Leukemia, 30 (12): 2364-2372. [PMID:27323910] |
3. Vercruysse T, De Bie J, Neggers JE, Jacquemyn M, Vanstreels E, Schmid-Burgk JL, Hornung V, Baloglu E, Landesman Y, Senapedis W et al.. (2017)
The Second-Generation Exportin-1 Inhibitor KPT-8602 Demonstrates Potent Activity against Acute Lymphoblastic Leukemia. Clin Cancer Res, 23 (10): 2528-2541. [PMID:27780859] |