Drug Repurposing Patent Applications July–September 2019

Gerken T , Girard CA , Tung YC , et al.: The obesity-associated FTO gene encodes a 2-oxoglutarate-dependent nucleic acid demethylase. Science, 2007; 318:1469–1472.

Scuteri A , Sanna S , Chen WM , et al.: Genome-wide association scan shows genetic variants in the FTO gene are associated with obesity-related traits. PLoS Genet, 2007; 3:e115.

Fischer J , Koch L , Emmerling C , et al.: Inactivation of the Fto gene protects from obesity. Nature, 2009; 458:894–898.

Doaei S , Mosavi Jarrahi SA , Sanjari Moghadam A , et al.: The effect of rs9930506 FTO gene polymorphism on obesity risk: a meta-analysis. Biomol Concepts, 2019; 10:237–242.

Ebell MH : Lorcaserin is safe, but only modestly effective for weight loss. Am Fam Physician 2019;99:Online. https://www.aafp.org/afp/2019/0315/od4.html (Last accessed January 29, 2020 ).

Ouchi M , Kitta T , Kanno Y , et al.: Effect of a 5-HT2c receptor agonist on urethral closure mechanisms in female rats. Neurourol Urodyn, 2018; 37:2382–2388.

Tolete P , Knupp K , Karlovich M , et al.: Lorcaserin therapy for severe epilepsy of childhood onset: a case series. Neurology, 2018; 91:837–839.

Pirtle JL , Hickman MD , Boinpelly VC , Surineni K , Thakur HK , Grasing KW : The serotonin-2C agonist Lorcaserin delays intravenous choice and modifies the subjective and cardiovascular effects of cocaine: a randomized, controlled human laboratory study. Pharmacol Biochem Behav, 2019; 180:52–59.

Kim SE , Kim JG , Park K : Biomaterials for the treatment of tendon injury. Tissue Eng Regen Med, 2019; 16:467–477.

Suzawa H , Kikuchi S , Arai N , Koda A : The mechanism involved in the inhibitory action of tranilast on collagen biosynthesis of keloid fibroblasts. Jpn J Pharmacol, 1992; 60:91–96.

Hu Z , Chen B , Li Y , et al.: Effect of tranilast on wound healing and administration time on scar hyperplasia of deep partial-thickness burn in mice. Zhongguo Xiu Fu Chong Jian Wai Ke Za Zhi, 2017; 31:465–472.

Liu Y , Kan M , Li A , et al.: Inhibitory effects of tranilast on cytokine, chemokine, adhesion molecule, and matrix metalloproteinase expression in human corneal fibroblasts exposed to Poly(I:C). Curr Eye Res, 2016; 41:1400–1407.

Shi TT , Yu XX , Yan LJ , Xiao HT . Research progress of hydroxychloroquine and autophagy inhibitors on cancer. Cancer Chemother Pharmacol, 2017; 79:287–294.

Cook KL , Wärri A , Soto-Pantoja DR , et al.: Hydroxychloroquine inhibits autophagy to potentiate antiestrogen responsiveness in ER+ breast cancer. Clin Cancer Res, 2014; 20:3222–3232. [Correction in: Clin Cancer Res 2016;20:2825].

Wang P , Du Y , Wang J : Identification of breast cancer subtypes sensitive to HCQ-induced autophagy inhibition. Pathol Res Pract, 2019; 215:152609.

Shukla AM , Shukla AW : Expanding horizons for clinical applications of chloroquine, hydroxychloroquine, and related structural analogues. Drugs Context, 2019; 8;pii:2019-9-1.

Hayashi G , Cortopassi G : Lymphoblast oxidative stress genes as potential biomarkers of disease severity and drug effect in Friedreich's ataxia. PLoS One, 2016; 11:e0153574.

Khdour OM , Bandyopadhyay I , Chowdhury SR , Visavadiya NP , Hecht SM : Lipophilic methylene blue analogues enhance mitochondrial function and increase frataxin levels in a cellular model of Friedreich's ataxia. Bioorg Med Chem, 2018; 26:3359–3369.

Bell KF , Claudio Cuello A : Altered synaptic function in Alzheimer's disease. Eur J Pharmacol, 2006; 545:11–21.

Chumakov I , Nabirotchkin S , Cholet N , et al.: Combining two repurposed drugs as a promising approach for Alzheimer's disease therapy. Sci Rep, 2015; 5:7608.

Tamir S , Paddock ML , Darash-Yahana-Baram M , et al.: Structure-function analysis of NEET proteins uncovers their role as key regulators of iron and ROS homeostasis in health and disease. Biochim Biophys Acta, 2015; 1853:1294–1315.

Karmi O , Marjault HB , Pesce L , et al.: The unique fold and lability of the [2Fe-2S] clusters of NEET proteins mediate their key functions in health and disease. J Biol Inorg Chem, 2018; 23:599–612.

Lipper CH , Karmi O , Sohn YS , et al.: Structure of the human monomeric NEET protein MiNT and its role in regulating iron and reactive oxygen species in cancer cells. Proc Natl Acad Sci USA, 2018; 115:272–277.

Geldenhuys WJ , Yonutas HM , Morris DL , Sullivan PG , Darvesh AS , Leeper TC : Identification of small molecules that bind to the mitochondrial protein mitoNEET. Bioorg Med Chem Lett, 2016; 26:5350–5353.

Kaplan JM , Zingarelli B , Krallman K , et al.: Phase 1 safety and pharmacokinetic study on the use of pioglitazone in critically ill patients with sepsis: a randomized clinical trial. Intensive Care Med, 2018; 44:2006–2008.

McCarthy CP , Mullins KV , Kerins DM : The role of trimetazidine in cardiovascular disease: beyond an anti-anginal agent. Eur Heart J Cardiovasc Pharmacother, 2016; 2:266–272.

Thadani U : Trimetazidine for stable and unstable ischemic heart diseases and for heart failure: is its routine use justified from available data?. Int J Cardiol, 2019; 300:45–46.

Yang Y , Li N , Chen T , Zhang C , Liu L , Qi Y , Bu P : Trimetazidine ameliorates sunitinib-induced cardiotoxicity in mice via the AMPK/mTOR/autophagy pathway. Pharm Biol, 2019; 57:625–631.

Karahan G , Kaya H , Erdogan MA , Yigitturk G , Gokyayla E , Erbas O : Effects of trimetazidine on nerve regeneration in a rat sciatic nerve injury model. Bratisl Lek Listy, 2019; 120:777–782.

Singh M , Alavi A , Wong R , Akita S : Radiodermatitis: a review of our current understanding. Am J Clin Dermatol, 2016; 17:277–292.

Ghebremariam YT , Cooke JP , Gerhart W , et al.: Pleiotropic effect of the proton pump inhibitor esomeprazole leading to suppression of lung inflammation and fibrosis. J Transl Med, 2015; 13:249.

Wang T , Hu P , Li B , Zhang JP , Cheng YF , Liang YM : Role of Nrf2 signaling pathway in the radiation tolerance of patients with head and neck squamous cell carcinoma: an in vivo and in vitro study. Onco Targets Ther, 2017; 10:1809–1819.

Pham N , Ludwig MS , Wang M , et al.: Topical esomeprazole mitigates radiation-induced dermal inflammation and fibrosis. Radiat Res, 2019; 192:473–482.

Young A , Namas R , Dodge C , Khanna D : Hand impairment in systemic sclerosis: various manifestations and currently available treatment. Curr Treatm Opt Rheumatol, 2016; 2:252–269.

Shipman L : Connective tissue diseases: digital ulcers unaffected by endothelin blockade. Nat Rev Rheumatol, 2016; 12:374.

de Vries-Bouwstra JK , Allanore Y , Matucci-Cerinic M , Balbir-Gurman A : Worldwide expert agreement on updated recommendations for the treatment of systemic sclerosis. J Rheumatol, 2019. [Epub ahead of print]; DOI: 10.3899/jrheum.181173.

Shi-Wen X , Denton CP , Dashwood MR , et al.: Fibroblast matrix gene expression and connective tissue remodeling: role of endothelin-1. J Invest Dermatol, 2001; 116:417–425.

Carrillo-Salinas FJ , Ngwenyama N , Anastasiou M , Kaur K , Alcaide P : Heart inflammation: immune cell roles and roads to the heart. Am J Pathol, 2019; 189:1482–1494.

Weirather J , Hofmann UD , Beyersdorf N , Ramos GC , Vogel B , Frey A : Foxp3+ CD4+ T cells improve healing after myocardial infarction by modulating monocyte/macrophage differentiation. Circ Res, 2014; 115:55–67.

Meng X , Yang J , Dong M , et al.: Regulatory T cells in cardiovascular diseases. Nat Rev Cardiol, 2016; 13:167–179.

Lai SL , Marín-Juez R , Moura PL , et al.: Reciprocal analyses in zebrafish and medaka reveal that harnessing the immune response promotes cardiac regeneration. Elife, 2017; 6:pii: e25605.

Brænne I , Zeng L , Willenborg C , et al.: Genomic correlates of glatiramer acetate adverse cardiovascular effects lead to a novel locus mediating coronary risk. PLoS One, 2017; 12:e0182999.

Kjaergaard N , Kjaergaard B , Lauritsen JG . Prazosin, an adrenergic blocking agent inadequate as male contraceptive pill. Contraception, 1988; 37:621–629.

Cakiroglu B , Hazar AI , Sinanoglu O , Arda E , Ekici S : Comparison of transurethral incision of the prostate and silodosin in patients having benign prostatic obstruction in terms of retrograde ejaculation. Arch Ital Urol Androl, 2017; 89:31–33.

Hisasue S , Furuya R , Itoh N , Kobayashi K , Furuya S , Tsukamoto T : Ejaculatory disorder caused by alpha-1 adrenoceptor antagonists is not retrograde ejaculation but a loss of seminal emission. Int J Urol, 2006; 13:1311–1316.

Bhat GS , Shastry A : A prospective double-blind, randomized, placebo-controlled study to evaluate the efficacy of silodosin 8 mg as an on-demand, reversible, nonhormonal oral contraceptive for males: a pilot study. World J Urol, 2019. [Epub ahead of print]; DOI: 10.1007/s00345-019-02806-7.