"目录号: HY-13690
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Mitotane(2,4′-DDD)是DDD的同分异构体和DDT的衍生物，有抗癌活性，可作用于肾上腺皮质癌。
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生物活性
Description
Mitotane(2,4′-DDD), an isomer of DDD and derivative of DDT, is an antineoplastic medication used in the treatment of adrenocortical carcinoma.IC50 value: Target: Mitotane alters steroid peripheral metabolism, directly suppresses the adrenal cortex and alters cortisone metabolism leading to hypocortisolism. Side effects as reported by Schteinberg et al. include anorexia and nausea (88%), diarrhea (38%), vomiting (23%), decreased memory and ability to concentrate (50%), rash (23%), gynecomastia (50%), arthralgia (19%), and leukopenia (7%).
Clinical Trial
NCT00777244
University of Turin, Italy
Adrenocortical Carcinoma
April 2008
Phase 3
NCT02057237
University Health Network, Toronto
Prostate Cancer
September 2013
Phase 1
NCT00778817
National Cancer Institute (NCI)
Recurrent Adrenocortical Carcinoma-Stage III Adrenocortical Carcinoma-Stage IV Adrenocortical Carcinoma
December 2008
Phase 2
NCT00001339
National Cancer Institute (NCI)-National Institutes of Health Clinical Center (CC)
Adrenal Cortical Carcinoma
August 1993
Phase 2
NCT00094497
Collaborative Group for Adrenocortical Carcinoma Treatment-German Federal Ministry of Education and Research-National Cancer Institute (NCI)
Carcinoma, Adrenal Cortical
June 2004
Phase 3
NCT00304070
Children's Oncology Group-National Cancer Institute (NCI)
Stage I Adrenocortical Carcinoma-Stage II Adrenocortical Carcinoma-Stage III Adrenocortical Carcinoma-Stage IV Adrenocortical Carcinoma
September 2006
Phase 3
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References
[1].Gentilin E, Tagliati F, Terzolo M, Mitotane reduces human and mouse ACTH-secreting pituitary cell viability and function. J Endocrinol. 2013 Jul 29;218(3):275-285.
[2].Lehmann TP, Wrzesiński T, Jagodziński PP. The effect of mitotane on viability, steroidogenesis and gene expression in NCI H295R adrenocortical cells. Mol Med Rep. 2013 Mar;7(3):893-900.
[3].Takeshita A, Igarashi-Migitaka J, Koibuchi N, Mitotane induces CYP3A4 expression via activation of the steroid and xenobiotic receptor. J Endocrinol. 2013 Feb 15;216(3):297-305.
[4].Ederhy S, Cohen A, Dufaitre G, No evidence for relevant QT interval prolongation in mitotane-treated patients with adrenocortical carcinoma. J Endocrinol Invest. 2012 Nov;35(10):911-4.
[5].Alexandraki KI, Kaltsas GA, le Roux CW, Assessment of serum-free cortisol levels in patients with adrenocortical carcinoma treated with mitotane: a pilot study. Clin Endocrinol (Oxf). 2010 Mar;72(3):305-11.