Literature DB >> 20978926

Dermatologic side effects associated with the MEK 1/2 inhibitor selumetinib (AZD6244, ARRY-142886).

Yevgeniy Balagula1, Katherine Barth Huston, Klaus J Busam, Mario E Lacouture, Paul B Chapman, Patricia L Myskowski.   

Abstract

BACKGROUND: Selumetinib (AZD6244, ARRY-142886) is a second generation MEK inhibitor that is currently in clinical trials for various solid malignancies. MEK kinase inhibitors are associated with dermatologic toxicities. While reactions affecting the skin, hair and nails to other targeted agents, such as epidermal growth factor receptor inhibitors (EGFRIs) have been abundantly described in recent years, the dermatologic toxicities associated with MEK inhibitors have not been well characterized. Similarly, their management may present a challenge in clinical trials. We reviewed the clinical presentation, evolution and management of dermatologic toxicities associated with selumetinib.
METHODS: A retrospective review of medical records of 11 patients referred to the Dermatology Service with dermatologic toxicities secondary to selumetinib was performed. Data from two phase II trials in which selumetinib was used to treat advanced metastatic cutaneous, mucosal, or uveal melanomas were reviewed. Parameters studied included the time to onset, clinical presentation, histology and management. In addition, the clinical database was accessed to retrieve clinical photographs when available.
RESULTS: Eight patients received selumetinib suspension orally at 100 mg twice a day and three patients received a newer capsule formulation at the maximum tolerated dose of 75 mg with the same frequency. The following adverse effects were observed: papulopustular rash (100%), xerosis (36%), pruritus (45%), fissures (9%), telangiectasias (27%), hyperpigmentation (9%), alopecia (9%), angular cheilitis (9%), and paronychia (9%). In addition, secondary bacterial infection with Staphylococcus aureus was documented in 3 patients (27%).
CONCLUSIONS: Dermatologic side-effects associated with selumetinib were similar to those seen with epidermal growth factor receptor inhibitors (EGFRIs). Treatment approaches used for EGFRI-induced dermatologic reactions may be potentially utilized to manage those associated with selumetinib.

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Year:  2010        PMID: 20978926      PMCID: PMC5691597          DOI: 10.1007/s10637-010-9567-3

Source DB:  PubMed          Journal:  Invest New Drugs        ISSN: 0167-6997            Impact factor:   3.850


  21 in total

Review 1.  Dermatologic side effects associated with the epidermal growth factor receptor inhibitors.

Authors:  Anna Liza C Agero; Stephen W Dusza; Cristiane Benvenuto-Andrade; Klaus J Busam; Patricia Myskowski; Allan C Halpern
Journal:  J Am Acad Dermatol       Date:  2006-10       Impact factor: 11.527

2.  Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies.

Authors:  Patricia M Lorusso; Alex A Adjei; Mary Varterasian; Shirish Gadgeel; Joel Reid; David Y Mitchell; Lorelei Hanson; Pamela DeLuca; Laura Bruzek; Jill Piens; Peggy Asbury; Keri Van Becelaere; Roman Herrera; Judith Sebolt-Leopold; Mark B Meyer
Journal:  J Clin Oncol       Date:  2005-07-11       Impact factor: 44.544

Review 3.  Mechanisms of cutaneous toxicities to EGFR inhibitors.

Authors:  Mario E Lacouture
Journal:  Nat Rev Cancer       Date:  2006-10       Impact factor: 60.716

Review 4.  The EGF receptor - an essential regulator of multiple epidermal functions.

Authors:  M Jost; C Kari; U Rodeck
Journal:  Eur J Dermatol       Date:  2000 Oct-Nov       Impact factor: 3.328

Review 5.  HER1/EGFR inhibitor-associated rash: future directions for management and investigation outcomes from the HER1/EGFR inhibitor rash management forum.

Authors:  Román Pérez-Soler; Jean Pierre Delord; Allan Halpern; Karen Kelly; James Krueger; Bartomeu Massutí Sureda; Joachim von Pawel; Jennifer Temel; Salvatore Siena; Denis Soulières; Leonard Saltz; James Leyden
Journal:  Oncologist       Date:  2005-05

6.  Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor.

Authors:  Tammie C Yeh; Vivienne Marsh; Bryan A Bernat; Josh Ballard; Heidi Colwell; Ron J Evans; Janet Parry; Darin Smith; Barbara J Brandhuber; Stefan Gross; Allison Marlow; Brian Hurley; Joe Lyssikatos; Patrice A Lee; James D Winkler; Kevin Koch; Eli Wallace
Journal:  Clin Cancer Res       Date:  2007-03-01       Impact factor: 12.531

7.  Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer.

Authors:  John Rinehart; Alex A Adjei; Patricia M Lorusso; David Waterhouse; J Randolph Hecht; Ronald B Natale; Oday Hamid; Mary Varterasian; Peggy Asbury; Eric P Kaldjian; Stephen Gulyas; David Y Mitchell; Roman Herrera; Judith S Sebolt-Leopold; Mark B Meyer
Journal:  J Clin Oncol       Date:  2004-10-13       Impact factor: 44.544

Review 8.  Skin toxicities associated with epidermal growth factor receptor inhibitors.

Authors:  Tianhong Li; Roman Perez-Soler
Journal:  Target Oncol       Date:  2009-05-19       Impact factor: 4.493

9.  AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models.

Authors:  Barry R Davies; Armelle Logie; Jennifer S McKay; Paul Martin; Samantha Steele; Richard Jenkins; Mark Cockerill; Sue Cartlidge; Paul D Smith
Journal:  Mol Cancer Ther       Date:  2007-08       Impact factor: 6.261

10.  Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers.

Authors:  Alex A Adjei; Roger B Cohen; Wilbur Franklin; Clive Morris; David Wilson; Julian R Molina; Lorelei J Hanson; Lia Gore; Laura Chow; Stephen Leong; Lara Maloney; Gilad Gordon; Heidi Simmons; Allison Marlow; Kevin Litwiler; Suzy Brown; Gregory Poch; Katie Kane; Jerry Haney; S Gail Eckhardt
Journal:  J Clin Oncol       Date:  2008-04-07       Impact factor: 44.544

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  26 in total

1.  [Cutaneous side effects of medical tumor therapy].

Authors:  A Degen; M Alter; F Schenck; A Kapp; R Gutzmer
Journal:  Hautarzt       Date:  2011-06       Impact factor: 0.751

2.  Dropped head syndrome: report of three cases during treatment with a MEK inhibitor.

Authors:  Xi Chen; Gary K Schwartz; Lisa M DeAngelis; Thomas Kaley; Richard D Carvajal
Journal:  Neurology       Date:  2012-10-17       Impact factor: 9.910

Review 3.  Pruritus Associated with Targeted Anticancer Therapies and Their Management.

Authors:  Jennifer Wu; Mario E Lacouture
Journal:  Dermatol Clin       Date:  2018-07       Impact factor: 3.478

Review 4.  Cutaneous Complications of Targeted Melanoma Therapy.

Authors:  Emily de Golian; Bernice Y Kwong; Susan M Swetter; Silvina B Pugliese
Journal:  Curr Treat Options Oncol       Date:  2016-11

5.  [Cutaneous side effects of anti-tumor therapy with BRAF and MEK inhibitors].

Authors:  R Gutzmer; J C Hassel; K C Kähler; C Loquai; R Mössner; S Ugurel; L Zimmer; Für Komitee Kutane Nebenwirkungen Ado der das Ado
Journal:  Hautarzt       Date:  2014-07       Impact factor: 0.751

6.  Identification of an In Vivo MEK/WOX1 Complex as a Master Switch for Apoptosis in T Cell Leukemia.

Authors:  Hsin-Ping Lin; Jean-Yun Chang; Sing-Ru Lin; Ming-Hui Lee; Shenq-Shyang Huang; Li-Jin Hsu; Nan-Shan Chang
Journal:  Genes Cancer       Date:  2011-05

7.  CInQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo.

Authors:  Dong Joon Kim; Mee-Hyun Lee; Kanamata Reddy; Yani Li; Do Young Lim; Hua Xie; Sung-Young Lee; Young Il Yeom; Ann M Bode; Zigang Dong
Journal:  Carcinogenesis       Date:  2013-01-25       Impact factor: 4.944

8.  A Phase I Study of the Safety, Pharmacokinetics, and Pharmacodynamics of Combination Therapy with Refametinib plus Sorafenib in Patients with Advanced Cancer.

Authors:  Alex A Adjei; Donald A Richards; Anthony El-Khoueiry; Fadi Braiteh; Carlos H R Becerra; Joe J Stephenson; Aram F Hezel; Morris Sherman; Lawrence Garbo; Diane P Leffingwell; Cory Iverson; Jeffrey N Miner; Zancong Shen; Li-Tain Yeh; Sonny Gunawan; David M Wilson; Kimberly J Manhard; Prabhu Rajagopalan; Heiko Krissel; Neil J Clendeninn
Journal:  Clin Cancer Res       Date:  2015-12-07       Impact factor: 12.531

Review 9.  Dermatological adverse events from BRAF inhibitors: a growing problem.

Authors:  Viswanath Reddy Belum; Alyssa Fischer; Jennifer Nam Choi; Mario E Lacouture
Journal:  Curr Oncol Rep       Date:  2013-06       Impact factor: 5.075

Review 10.  [Drug reactions caused by chemotherapy agents].

Authors:  L M Ehmann; H Schrumpf; P A Gerber; B Homey
Journal:  Hautarzt       Date:  2014-05       Impact factor: 0.751

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