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Items: 1 to 20 of 110

1.

First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study.

Sullivan RJ, Infante JR, Janku F, Wong DJL, Sosman JA, Keedy V, Patel MR, Shapiro GI, Mier JW, Tolcher AW, Wang-Gillam A, Sznol M, Flaherty K, Buchbinder E, Carvajal RD, Varghese AM, Lacouture ME, Ribas A, Patel SP, DeCrescenzo GA, Emery CM, Groover AL, Saha S, Varterasian M, Welsch DJ, Hyman DM, Li BT.

Cancer Discov. 2018 Feb;8(2):184-195. doi: 10.1158/2159-8290.CD-17-1119. Epub 2017 Dec 15.

2.

Effect of ulixertinib, a novel ERK1/2 inhibitor, on the QT/QTc interval in patients with advanced solid tumor malignancies.

Mendzelevski B, Ferber G, Janku F, Li BT, Sullivan RJ, Welsch D, Chi W, Jackson J, Weng O, Sager PT.

Cancer Chemother Pharmacol. 2018 Jun;81(6):1129-1141. doi: 10.1007/s00280-018-3564-1. Epub 2018 Mar 30.

3.

Development of MK-8353, an orally administered ERK1/2 inhibitor, in patients with advanced solid tumors.

Moschos SJ, Sullivan RJ, Hwu WJ, Ramanathan RK, Adjei AA, Fong PC, Shapira-Frommer R, Tawbi HA, Rubino J, Rush TS 3rd, Zhang D, Miselis NR, Samatar AA, Chun P, Rubin EH, Schiller J, Long BJ, Dayananth P, Carr D, Kirschmeier P, Bishop WR, Deng Y, Cooper A, Shipps GW, Moreno BH, Robert L, Ribas A, Flaherty KT.

JCI Insight. 2018 Feb 22;3(4). pii: 92352. doi: 10.1172/jci.insight.92352. eCollection 2018 Feb 22.

4.

First-in-human, open-label dose-escalation and dose-expansion study of the safety, pharmacokinetics, and antitumor effects of an oral ALK inhibitor ASP3026 in patients with advanced solid tumors.

Li T, LoRusso P, Maitland ML, Ou SH, Bahceci E, Ball HA, Park JW, Yuen G, Tolcher A.

J Hematol Oncol. 2016 Mar 10;9:23. doi: 10.1186/s13045-016-0254-5.

5.

A first-in-human phase I study to evaluate the MEK1/2 inhibitor, cobimetinib, administered daily in patients with advanced solid tumors.

Rosen LS, LoRusso P, Ma WW, Goldman JW, Weise A, Colevas AD, Adjei A, Yazji S, Shen A, Johnston S, Hsieh HJ, Chan IT, Sikic BI.

Invest New Drugs. 2016 Oct;34(5):604-13. doi: 10.1007/s10637-016-0374-3. Epub 2016 Jul 16.

6.

Concurrent HER or PI3K Inhibition Potentiates the Antitumor Effect of the ERK Inhibitor Ulixertinib in Preclinical Pancreatic Cancer Models.

Jiang H, Xu M, Li L, Grierson P, Dodhiawala P, Highkin M, Zhang D, Li Q, Wang-Gillam A, Lim KH.

Mol Cancer Ther. 2018 Oct;17(10):2144-2155. doi: 10.1158/1535-7163.MCT-17-1142. Epub 2018 Jul 31.

7.

Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib).

Germann UA, Furey BF, Markland W, Hoover RR, Aronov AM, Roix JJ, Hale M, Boucher DM, Sorrell DA, Martinez-Botella G, Fitzgibbon M, Shapiro P, Wick MJ, Samadani R, Meshaw K, Groover A, DeCrescenzo G, Namchuk M, Emery CM, Saha S, Welsch DJ.

Mol Cancer Ther. 2017 Nov;16(11):2351-2363. doi: 10.1158/1535-7163.MCT-17-0456. Epub 2017 Sep 22.

8.

First-in-Man Dose-Escalation Study of the Selective BRAF Inhibitor RG7256 in Patients with BRAF V600-Mutated Advanced Solid Tumors.

Dienstmann R, Lassen U, Cebon J, Desai J, Brown MP, Evers S, Su F, Zhang W, Boisserie F, Lestini B, Schostack K, Meresse V, Tabernero J.

Target Oncol. 2016 Apr;11(2):149-56. doi: 10.1007/s11523-015-0381-x.

PMID:
26310975
9.

Phase I expansion and pharmacodynamic study of the oral MEK inhibitor RO4987655 (CH4987655) in selected patients with advanced cancer with RAS-RAF mutations.

Zimmer L, Barlesi F, Martinez-Garcia M, Dieras V, Schellens JH, Spano JP, Middleton MR, Calvo E, Paz-Ares L, Larkin J, Pacey S, Venturi M, Kraeber-Bodéré F, Tessier JJ, Eberhardt WE, Paques M, Guarin E, Meresse V, Soria JC.

Clin Cancer Res. 2014 Aug 15;20(16):4251-61. doi: 10.1158/1078-0432.CCR-14-0341. Epub 2014 Jun 19.

10.

A phase I, dose-escalation study of the multitargeted receptor tyrosine kinase inhibitor, golvatinib, in patients with advanced solid tumors.

Molife LR, Dean EJ, Blanco-Codesido M, Krebs MG, Brunetto AT, Greystoke AP, Daniele G, Lee L, Kuznetsov G, Myint KT, Wood K, de Las Heras B, Ranson MR.

Clin Cancer Res. 2014 Dec 15;20(24):6284-94. doi: 10.1158/1078-0432.CCR-14-0409. Epub 2014 Oct 2.

11.

Phase I Dose-Escalation and -Expansion Study of the BRAF Inhibitor Encorafenib (LGX818) in Metastatic BRAF-Mutant Melanoma.

Delord JP, Robert C, Nyakas M, McArthur GA, Kudchakar R, Mahipal A, Yamada Y, Sullivan R, Arance A, Kefford RF, Carlino MS, Hidalgo M, Gomez-Roca C, Michel D, Seroutou A, Aslanis V, Caponigro G, Stuart DD, Moutouh-de Parseval L, Demuth T, Dummer R.

Clin Cancer Res. 2017 Sep 15;23(18):5339-5348. doi: 10.1158/1078-0432.CCR-16-2923. Epub 2017 Jun 13.

12.

A phase I pharmacokinetic and pharmacodynamic study of the oral mitogen-activated protein kinase kinase (MEK) inhibitor, WX-554, in patients with advanced solid tumours.

Jamieson D, Griffin MJ, Sludden J, Drew Y, Cresti N, Swales K, Merriman M, Allen R, Bevan P, Buerkle M, Mala C, Coyle V, Rodgers L, Dean E, Greystoke A, Banerji U, Wilson RH, Evans TR, Anthoney A, Ranson M, Boddy AV, Plummer R.

Eur J Cancer. 2016 Nov;68:1-10. doi: 10.1016/j.ejca.2016.08.026. Epub 2016 Sep 28.

PMID:
27693888
13.

Combination of vemurafenib and cobimetinib in patients with advanced BRAF(V600)-mutated melanoma: a phase 1b study.

Ribas A, Gonzalez R, Pavlick A, Hamid O, Gajewski TF, Daud A, Flaherty L, Logan T, Chmielowski B, Lewis K, Kee D, Boasberg P, Yin M, Chan I, Musib L, Choong N, Puzanov I, McArthur GA.

Lancet Oncol. 2014 Aug;15(9):954-65. doi: 10.1016/S1470-2045(14)70301-8. Epub 2014 Jul 15. Erratum in: Lancet Oncol. 2014 Sep;15(10):417.

PMID:
25037139
14.

Multicenter phase I trial of the mitogen-activated protein kinase 1/2 inhibitor BAY 86-9766 in patients with advanced cancer.

Weekes CD, Von Hoff DD, Adjei AA, Leffingwell DP, Eckhardt SG, Gore L, Lewis KD, Weiss GJ, Ramanathan RK, Dy GK, Ma WW, Sheedy B, Iverson C, Miner JN, Shen Z, Yeh LT, Dubowy RL, Jeffers M, Rajagopalan P, Clendeninn NJ.

Clin Cancer Res. 2013 Mar 1;19(5):1232-43. doi: 10.1158/1078-0432.CCR-12-3529. Epub 2013 Feb 22.

15.

Efficacy and Safety of Abemaciclib, an Inhibitor of CDK4 and CDK6, for Patients with Breast Cancer, Non-Small Cell Lung Cancer, and Other Solid Tumors.

Patnaik A, Rosen LS, Tolaney SM, Tolcher AW, Goldman JW, Gandhi L, Papadopoulos KP, Beeram M, Rasco DW, Hilton JF, Nasir A, Beckmann RP, Schade AE, Fulford AD, Nguyen TS, Martinez R, Kulanthaivel P, Li LQ, Frenzel M, Cronier DM, Chan EM, Flaherty KT, Wen PY, Shapiro GI.

Cancer Discov. 2016 Jul;6(7):740-53. doi: 10.1158/2159-8290.CD-16-0095. Epub 2016 May 23.

16.

ERK Inhibition: A New Front in the War against MAPK Pathway-Driven Cancers?

Smalley I, Smalley KSM.

Cancer Discov. 2018 Feb;8(2):140-142. doi: 10.1158/2159-8290.CD-17-1355.

17.

Phase I and pharmacokinetics/pharmacodynamics study of the MEK inhibitor RO4987655 in Japanese patients with advanced solid tumors.

Nakamichi S, Nokihara H, Yamamoto N, Yamada Y, Fujiwara Y, Tamura Y, Wakui H, Honda K, Mizugaki H, Kitazono S, Tanabe Y, Asahina H, Yamazaki N, Suzuki S, Matsuoka M, Ogita Y, Tamura T.

Invest New Drugs. 2015 Jun;33(3):641-51. doi: 10.1007/s10637-015-0229-3. Epub 2015 Mar 27.

PMID:
25809858
18.

A phase I study of binimetinib (MEK162) in Japanese patients with advanced solid tumors.

Watanabe K, Otsu S, Hirashima Y, Morinaga R, Nishikawa K, Hisamatsu Y, Shimokata T, Inada-Inoue M, Shibata T, Takeuchi H, Watanabe T, Tokushige K, Maacke H, Shiaro K, Ando Y.

Cancer Chemother Pharmacol. 2016 Jun;77(6):1157-64. doi: 10.1007/s00280-016-3019-5. Epub 2016 Apr 12.

PMID:
27071922
19.

A phase Ib dose-escalation study of the oral pan-PI3K inhibitor buparlisib (BKM120) in combination with the oral MEK1/2 inhibitor trametinib (GSK1120212) in patients with selected advanced solid tumors.

Bedard PL, Tabernero J, Janku F, Wainberg ZA, Paz-Ares L, Vansteenkiste J, Van Cutsem E, Pérez-García J, Stathis A, Britten CD, Le N, Carter K, Demanse D, Csonka D, Peters M, Zubel A, Nauwelaerts H, Sessa C.

Clin Cancer Res. 2015 Feb 15;21(4):730-8. doi: 10.1158/1078-0432.CCR-14-1814. Epub 2014 Dec 10.

20.

A Multicenter Phase I Study Evaluating Dual PI3K and BRAF Inhibition with PX-866 and Vemurafenib in Patients with Advanced BRAF V600-Mutant Solid Tumors.

Yam C, Xu X, Davies MA, Gimotty PA, Morrissette JJD, Tetzlaff MT, Wani KM, Liu S, Deng W, Buckley M, Zhao J, Amaravadi RK, Haas NB, Kudchadkar RR, Pavlick AC, Sosman JA, Tawbi H, Walker L, Schuchter LM, Karakousis GC, Gangadhar TC.

Clin Cancer Res. 2018 Jan 1;24(1):22-32. doi: 10.1158/1078-0432.CCR-17-1807. Epub 2017 Oct 19.

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