Rethinking tamoxifen in the management of melanoma: New answers for an old question

Ribeiro, Mariana P.C.; Santos, Ana Lúcia; Custódio, José B.A.

doi:10.1016/j.ejphar.2015.07.023

Cited by 12 publications

(12 citation statements)

References 93 publications

(98 reference statements)

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“…To our knowledge apart from our study, only a recently mentioned unpublished observation described GPER in melanoma using a mouse cell line model. 70 Here, we also showed that in the majority of GPER-positive melanomas, ERb was also present (39/41) and this double receptor expression was associated with favourable disease prognostic markers such as lower Breslow thickness, lower mitotic rate, higher presence of PLI, indicating a better DFS. Co-expression of ERb and GPER was described in advanced disease stage uterine carcinosarcomas, 71 and also in human ovarian cancer cell line, where GPER stimulated the cell proliferation ligand-independent manner.…”

Section: Discussionsupporting

confidence: 72%

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Expression of G protein‐coupled oestrogen receptor in melanoma and in pregnancy‐associated melanoma

Fábián

Rencz

Krenács

et al. 2017

Acad Dermatol Venereol

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Section: Discussionsupporting

confidence: 72%

“…Although GPER expression was more common in PAM group, in multivariate analysis, there was no significant difference in DFS between PAM and NPAM patients. To our knowledge apart from our study, only a recently mentioned unpublished observation described GPER in melanoma using a mouse cell line model …”

Section: Discussionmentioning

confidence: 88%

Expression of G protein‐coupled oestrogen receptor in melanoma and in pregnancy‐associated melanoma

Fábián

Rencz

Krenács

et al. 2017

Acad Dermatol Venereol

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“…TAM's clinical efficacy, at least in part, depends on its metabolization in the liver, resulting in variable concentrations of active metabolites in the patient plasma. Therefore, to induce melanoma cell death in vitro, endoxifen (EDX), a metabolite of TAM that is safer and has more cytostatic activity than the parent drug has been used [66]. Furthermore, EDX orally administered in mice for four weeks reduced lung metastatic nodules without any side effects [57].…”

Section: Female Hormone Activitymentioning

confidence: 99%

Sex and Gender Disparities in Melanoma

Bellenghi

Puglisi

Pontecorvi

et al. 2020

Cancers

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Worldwide, the total incidence of cutaneous melanoma is higher in men than in women, with some differences related to ethnicity and age and, above all, sex and gender. Differences exist in respect to the anatomic localization of melanoma, in that it is more frequent on the trunk in men and on the lower limbs in women. A debated issue is if—and to what extent—melanoma development can be attributed to gender-specific behaviors or to biologically intrinsic differences. In the search for factors responsible for the divergences, a pivotal role of sex hormones has been observed, although conflicting results indicate the involvement of other mechanisms. The presence on the X chromosome of numerous miRNAs and coding genes playing immunological roles represents another important factor, whose relevance can be even increased by the incomplete X chromosome random inactivation. Considering the known advantages of the female immune system, a different cancer immune surveillance efficacy was suggested to explain some sex disparities. Indeed, the complexity of this picture emerged when the recently developed immunotherapies unexpectedly showed better improvements in men than in women. Altogether, these data support the necessity of further studies, which consider enrolling a balanced number of men and women in clinical trials to better understand the differences and obtain actual gender-equitable healthcare.

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“…With the growth in understanding of the importance of cytochrome P450 2D6 (CYP2D6) polymorphism and its relationship with the therapeutic outcome of tamoxifen in patients with breast cancer [ 6 ], we can now partly attribute the unpredictable results from early melanoma studies to CYP2D6 polymorphism [ 7 ]. Drug–drug interactions have also been shown to affect tamoxifen activity.…”

Section: Introductionmentioning

confidence: 99%

Orally administered endoxifen inhibits tumor growth in melanoma-bearing mice

Chen¹,

Sheikh²,

Ahmad³

et al. 2018

Cell Mol Biol Lett

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Endoxifen, an active metabolite of tamoxifen, has been shown to be an effective anti-estrogenic agent in estrogen receptor-positive breast cancer patients. In melanoma, estrogen receptor expression is shown to be associated with disease progression. However, the therapeutic benefit of endoxifen in melanoma has not yet been evaluated. Here, we present the first demonstration of the anti-melanogenic activity of endoxifen in vitro and in vivo.The in vitro cytotoxic effect of endoxifen was tested using a cell viability assay. The in vivo anti-melanogenic activity was evaluated in B16F10 cell-bearing C57BL/6 mice, a mouse melanoma model. The general toxicity was tested in Swiss albino mice.Endoxifen exhibited greater activity against melanoma cell lines. Treatment of B16F10 mouse and SK-MEL-5 human melanoma cell lines with 10 μM of endoxifen for 48 h respectively resulted in 93.6 and 92.5% cell death. Orally administered endoxifen, at dose levels of 4 and 8 mg/kg body weight/day for 20 consecutive days, respectively reduced metastatic melanoma nodules in the lungs by 26.7 and 82.7%.Endoxifen was found to be a safe and effective anti-melanogenic agent in animal studies.

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Rethinking tamoxifen in the management of melanoma: New answers for an old question

Cited by 12 publications

References 93 publications

Expression of G protein‐coupled oestrogen receptor in melanoma and in pregnancy‐associated melanoma

Expression of G protein‐coupled oestrogen receptor in melanoma and in pregnancy‐associated melanoma

Sex and Gender Disparities in Melanoma

Orally administered endoxifen inhibits tumor growth in melanoma-bearing mice

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