Alitretinoin: a comprehensive review

Cheng, Caleb; Michaels, Jason; Scheinfeld, Noah

doi:10.1517/13543784.17.3.437

Cited by 76 publications

(51 citation statements)

References 19 publications

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“…It is a pan-RAR, pan-RXR receptor agonist. 46 Studies are needed to determine the relative effectiveness of ATRA versus alitretinoin in RIG upregulation and HCV suppression and IFNa augmentation in treating IFN sensitive cancers.…”

Section: Amplification Elementsmentioning

confidence: 99%

Potential for all-trans retinoic acid [tretinoin] to enhance interferon-alpha treatment response in chronic myelogenous leukemia, melanoma, myeloma, and renal cell carcinoma

Kast¹

2008

Cancer Biology & Therapy

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Section: Amplification Elementsmentioning

confidence: 99%

Potential for all-trans retinoic acid [tretinoin] to enhance interferon-alpha treatment response in chronic myelogenous leukemia, melanoma, myeloma, and renal cell carcinoma

Kast¹

2008

Cancer Biology & Therapy

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“…As a panagonist of six nuclear receptors, 9cRA has undergone extensive pharmacological assessment. As the drug alitretinoin, it is effective against chronic hand dermatitis and Tcell lymphoma (14). Used systemically, it alters energy metabolism (15).…”

mentioning

confidence: 99%

Identification of 9- cis -retinoic acid as a pancreas-specific autacoid that attenuates glucose-stimulated insulin secretion

Kane

Folias

Pingitore

et al. 2010

Proc. Natl. Acad. Sci. U.S.A.

100

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The all-trans-retinoic acid (atRA) isomer, 9-cis-retinoic acid (9cRA), activates retinoic acid receptors (RARs) and retinoid X receptors (RXRs) in vitro. RARs control multiple genes, whereas RXRs serve as partners for RARs and other nuclear receptors that regulate metabolism. Physiological function has not been determined for 9cRA, because it has not been detected in serum or multiple tissues with analytically validated assays. Here, we identify 9cRA in mouse pancreas by liquid chromatography/tandem mass spectrometry (LC/MS/MS), and show that 9cRA decreases with feeding and after glucose dosing and varies inversely with serum insulin. 9cRA reduces glucose-stimulated insulin secretion (GSIS) in mouse islets and in the rat β-cell line 832/13 within 15 min by reducing glucose transporter type 2 (Glut2) and glucokinase (GK) activities. 9cRA also reduces Pdx-1 and HNF4α mRNA expression, ∼8-and 80-fold, respectively: defects in Pdx-1 or HNF4α cause maturity onset diabetes of the young (MODY4 and 1, respectively), as does a defective GK gene (MODY2). Pancreas β-cells generate 9cRA, and mouse models of reduced β-cell number, heterozygous Akita mice, and streptozotocin-treated mice have reduced 9cRA. 9cRA is abnormally high in glucose-intolerant mice, which have β-cell hypertropy, including mice with diet-induced obesity (DIO) and ob/ob and db/db mice. These data establish 9cRA as a pancreas-specific autacoid with multiple mechanisms of action and provide unique insight into GSIS.retinol | vitamin A | rexinoids I mpaired glucose-stimulated insulin secretion (GSIS) develops through multiple mechanisms, including actions of metabolic hormones and inflammatory cytokines, products of metabolic overload, and endoplasmic reticulum stress; however, mechanisms of GSIS and impaired glucose tolerance remain incompletely understood (1-4). Also uncertain is the contribution of impaired glucose tolerance to diminished pancreatic β-cell function and mass associated with type 2 diabetes (5). GSIS relies on the pancreas, and pancreas development, islet formation, and function require normal vitamin A nutriture (6-8). Vitamin A restriction during development impairs islet development and promotes glucose intolerance in adult rodents. On the other hand, restricting vitamin A in mature diabetes-prone rats reduces diabetes and insulitis, possibly through enhancing glucose sensing and metabolism. Alltrans-retinoic acid (atRA), an activated metabolite of vitamin A, regulates pancreas development, and atRA does not enhance the incidence of diabetes in diabetes-prone rats fed a vitamin Adeficient diet (7, 9, 10). Although the contribution of vitamin A to pancreas development through atRA seems clear, mechanisms whereby vitamin A affects mature pancreas function have not been determined in depth, nor have the specific vitamin A metabolites been identified that contribute to GSIS control.atRA induces differentiation and regulates cell processes by activating the nuclear receptors RAR α, -β, and -γ, which regulate transcription and translation (11...

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“…The most frequent retinoid receptor in the skin is RAR-γ/RXR-α heterodimer [1] . Previously used retinoids (such as acitretin and etretinate) target mainly RAR receptors.…”

Section: Discussionmentioning

confidence: 99%

Successful Treatment of Recalcitrant Prurigo with Alitretinoin

Gadaldi

Erdemoglu²,

Yawalkar³

2015

Dermatology

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Background: Chronic itch with secondary scratch lesions such as prurigo has a major impact on quality of life. Due to its relapsing nature and often unknown origin, its treatment is challenging. Objective: We sought to demonstrate that alitretinoin can be an efficacious and well-tolerated treatment in a patient suffering from chronic itch with concomitant prurigo and psoriatic lesions. Methods: Case report. Results: After 1 month of alitretinoin treatment (30 mg daily), itch as well as prurigo and psoriasis lesions decreased markedly. Three cycles of alitretinoin were administered, as each cessation of treatment led to relapse of the symptoms after 6-8 weeks. Tapering of the alitretinoin dose (30 mg every second day) after the third cycle allowed to maintain the effects for over 18 months. Conclusion: Treatment of refractory prurigo with alitretinoin might be an efficacious alternative to standard therapies. In case of relapse, retreatment with alitretinoin reinduces a further long-lasting response.

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Alitretinoin: a comprehensive review

Cited by 76 publications

References 19 publications

Potential for all-trans retinoic acid [tretinoin] to enhance interferon-alpha treatment response in chronic myelogenous leukemia, melanoma, myeloma, and renal cell carcinoma

Potential for all-trans retinoic acid [tretinoin] to enhance interferon-alpha treatment response in chronic myelogenous leukemia, melanoma, myeloma, and renal cell carcinoma

Identification of 9- cis -retinoic acid as a pancreas-specific autacoid that attenuates glucose-stimulated insulin secretion

Successful Treatment of Recalcitrant Prurigo with Alitretinoin

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