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Phospho-valproic acid (MDC-1112) reduces pancreatic cancer growth in patient-derived tumor xenografts and KPC mice: enhanced efficacy when combined with gemcitabine.

Luo D, DiGiovanni MG, Wei R, LaComb JF, Williams JL, Rigas B, Mackenzie GG.

Carcinogenesis. 2019 Oct 4. pii: bgz170. doi: 10.1093/carcin/bgz170. [Epub ahead of print]


NSAID-induced corneal melt: Clinical importance, pathogenesis, and risk mitigation.

Rigas B, Huang W, Honkanen R.

Surv Ophthalmol. 2019 Jul 12. pii: S0039-6257(19)30049-9. doi: 10.1016/j.survophthal.2019.07.001. [Epub ahead of print] Review.


Phospho-valproic acid (MDC-1112) suppresses glioblastoma growth in preclinical models through the inhibition of STAT3 phosphorylation.

Luo D, Fraga-Lauhirat M, Millings J, Ho C, Villarreal EM, Fletchinger TC, Bonfiglio JV, Mata L, Nemesure MD, Bartels LE, Wang R, Rigas B, Mackenzie GG.

Carcinogenesis. 2019 Apr 17. pii: bgz069. doi: 10.1093/carcin/bgz069. [Epub ahead of print]


A New Rabbit Model of Chronic Dry Eye Disease Induced by Complete Surgical Dacryoadenectomy.

Honkanen R, Huang W, Huang L, Kaplowitz K, Weissbart S, Rigas B.

Curr Eye Res. 2019 Aug;44(8):863-872. doi: 10.1080/02713683.2019.1594933. Epub 2019 Apr 15.


The ocular pharmacokinetics and biodistribution of phospho-sulindac (OXT-328) formulated in nanoparticles: Enhanced and targeted tissue drug delivery.

Wen Z, Muratomi N, Huang W, Huang L, Ren J, Yang J, Persaud Y, Loloi J, Mallangada N, Kung P, Honkanen R, Rigas B.

Int J Pharm. 2019 Feb 25;557:273-279. doi: 10.1016/j.ijpharm.2018.12.057. Epub 2018 Dec 28.


The Chemoprevention of Ovarian Cancer: the Need and the Options.

Kathawala RJ, Kudelka A, Rigas B.

Curr Pharmacol Rep. 2018;4(3):250-260. doi: 10.1007/s40495-018-0133-6. Epub 2018 May 2. Review. Erratum in: Curr Pharmacol Rep. 2018;4(5):414.


Phosphosulindac is efficacious in an improved concanavalin A-based rabbit model of chronic dry eye disease.

Honkanen RA, Huang L, Xie G, Rigas B.

Transl Res. 2018 Aug;198:58-72. doi: 10.1016/j.trsl.2018.04.002. Epub 2018 Apr 10.


Correction: The Chemoprevention of Ovarian Cancer: the Need and the Options.

Kathawala RJ, Kudelka A, Rigas B.

Curr Pharmacol Rep. 2018;4(5):414. doi: 10.1007/s40495-018-0159-9. Epub 2018 Sep 10.


Alkaline Ceramidase 1 Protects Mice from Premature Hair Loss by Maintaining the Homeostasis of Hair Follicle Stem Cells.

Lin CL, Xu R, Yi JK, Li F, Chen J, Jones EC, Slutsky JB, Huang L, Rigas B, Cao J, Zhong X, Snider AJ, Obeid LM, Hannun YA, Mao C.

Stem Cell Reports. 2017 Nov 14;9(5):1488-1500. doi: 10.1016/j.stemcr.2017.09.015. Epub 2017 Oct 19.


Phospho-valproic acid inhibits pancreatic cancer growth in mice: enhanced efficacy by its formulation in poly-(L)-lactic acid-poly(ethylene glycol) nanoparticles.

Mattheolabakis G, Wang R, Rigas B, Mackenzie GG.

Int J Oncol. 2017 Oct;51(4):1035-1044. doi: 10.3892/ijo.2017.4103. Epub 2017 Aug 25. Erratum in: Int J Oncol. 2018 Dec;53(6):2800.


Phospho-Aspirin (MDC-22) Prevents Pancreatic Carcinogenesis in Mice.

Mattheolabakis G, Papayannis I, Yang J, Vaeth BM, Wang R, Bandovic J, Ouyang N, Rigas B, Mackenzie GG.

Cancer Prev Res (Phila). 2016 Jul;9(7):624-34. doi: 10.1158/1940-6207.CAPR-15-0344. Epub 2016 May 2.


The novel agent phospho-glycerol-ibuprofen-amide (MDC-330) inhibits glioblastoma growth in mice: an effect mediated by cyclin D1.

Bartels LE, Mattheolabakis G, Vaeth BM, LaComb JF, Wang R, Zhi J, Komninou D, Rigas B, Mackenzie GG.

Carcinogenesis. 2016 Apr;37(4):420-429. doi: 10.1093/carcin/bgw017. Epub 2016 Feb 10.


NSAIDs and Colorectal Cancer Control: Promise and Challenges.

Tsioulias GJ, Go MF, Rigas B.

Curr Pharmacol Rep. 2015 Oct 1;1(5):295-301. Epub 2015 May 14.


Altered Interactions between the Gut Microbiome and Colonic Mucosa Precede Polyposis in APCMin/+ Mice.

Son JS, Khair S, Pettet DW 3rd, Ouyang N, Tian X, Zhang Y, Zhu W, Mackenzie GG, Robertson CE, Ir D, Frank DN, Rigas B, Li E.

PLoS One. 2015 Jun 29;10(6):e0127985. doi: 10.1371/journal.pone.0127985. eCollection 2015.


Repurposing the antipsychotic trifluoperazine as an antimetastasis agent.

Pulkoski-Gross A, Li J, Zheng C, Li Y, Ouyang N, Rigas B, Zucker S, Cao J.

Mol Pharmacol. 2015;87(3):501-12. doi: 10.1124/mol.114.096941. Epub 2014 Dec 31.


Phospho-NSAIDs have enhanced efficacy in mice lacking plasma carboxylesterase: implications for their clinical pharmacology.

Wong CC, Cheng KW, Papayannis I, Mattheolabakis G, Huang L, Xie G, Ouyang N, Rigas B.

Pharm Res. 2015 May;32(5):1663-75. doi: 10.1007/s11095-014-1565-2. Epub 2014 Nov 13.


Phospho-aspirin-2 (MDC-22) inhibits estrogen receptor positive breast cancer growth both in vitro and in vivo by a redox-dependent effect.

Huang L, Wong CC, Cheng KW, Rigas B.

PLoS One. 2014 Nov 4;9(11):e111720. doi: 10.1371/journal.pone.0111720. eCollection 2014.


A novel ibuprofen derivative with anti-lung cancer properties: synthesis, formulation, pharmacokinetic and efficacy studies.

Cheng KW, Nie T, Ouyang N, Alston N, Wong CC, Mattheolabakis G, Papayannis I, Huang L, Rigas B.

Int J Pharm. 2014 Dec 30;477(1-2):236-43. doi: 10.1016/j.ijpharm.2014.10.019. Epub 2014 Oct 11.


Pegylation improves the pharmacokinetics and bioavailability of small-molecule drugs hydrolyzable by esterases: a study of phospho-Ibuprofen.

Mattheolabakis G, Wong CC, Sun Y, Amella CA, Richards R, Constantinides PP, Rigas B.

J Pharmacol Exp Ther. 2014 Oct;351(1):61-6. doi: 10.1124/jpet.114.217208. Epub 2014 Jul 21.


The in vitro metabolism of phospho-sulindac amide, a novel potential anticancer agent.

Xie G, Cheng KW, Huang L, Rigas B.

Biochem Pharmacol. 2014 Sep 15;91(2):249-55. doi: 10.1016/j.bcp.2014.07.007. Epub 2014 Jul 18.


Phospho-aspirin (MDC-22) inhibits breast cancer in preclinical animal models: an effect mediated by EGFR inhibition, p53 acetylation and oxidative stress.

Huang L, Wong CC, Mackenzie GG, Sun Y, Cheng KW, Vrankova K, Alston N, Ouyang N, Rigas B.

BMC Cancer. 2014 Feb 28;14:141. doi: 10.1186/1471-2407-14-141.


Phospho-sulindac inhibits pancreatic cancer growth: NFATc1 as a drug resistance candidate.

Murray OT, Wong CC, Vrankova K, Rigas B.

Int J Oncol. 2014 Feb;44(2):521-9. doi: 10.3892/ijo.2013.2190. Epub 2013 Nov 27.


A novel Ras inhibitor (MDC-1016) reduces human pancreatic tumor growth in mice.

Mackenzie GG, Bartels LE, Xie G, Papayannis I, Alston N, Vrankova K, Ouyang N, Rigas B.

Neoplasia. 2013 Oct;15(10):1184-95.


Curcumin enhances the lung cancer chemopreventive efficacy of phospho-sulindac by improving its pharmacokinetics.

Cheng KW, Wong CC, Mattheolabakis G, Xie G, Huang L, Rigas B.

Int J Oncol. 2013 Sep;43(3):895-902. doi: 10.3892/ijo.2013.1995. Epub 2013 Jun 27.


Targeting mitochondrial STAT3 with the novel phospho-valproic acid (MDC-1112) inhibits pancreatic cancer growth in mice.

Mackenzie GG, Huang L, Alston N, Ouyang N, Vrankova K, Mattheolabakis G, Constantinides PP, Rigas B.

PLoS One. 2013 May 1;8(5):e61532. doi: 10.1371/journal.pone.0061532. Print 2013.


Aerosol administration of phospho-sulindac inhibits lung tumorigenesis.

Cheng KW, Wong CC, Alston N, Mackenzie GG, Huang L, Ouyang N, Xie G, Wiedmann T, Rigas B.

Mol Cancer Ther. 2013 Aug;12(8):1417-28. doi: 10.1158/1535-7163.MCT-13-0006-T. Epub 2013 May 3.


Topically applied phospho-sulindac hydrogel is efficacious and safe in the treatment of experimental arthritis in rats.

Mattheolabakis G, Mackenzie GG, Huang L, Ouyang N, Cheng KW, Rigas B.

Pharm Res. 2013 Jun;30(6):1471-82. doi: 10.1007/s11095-012-0953-8. Epub 2013 Mar 13.


Comparative in vitro metabolism of phospho-tyrosol-indomethacin by mice, rats and humans.

Xie G, Zhou D, Cheng KW, Wong CC, Rigas B.

Biochem Pharmacol. 2013 Apr 15;85(8):1195-202. doi: 10.1016/j.bcp.2013.01.031. Epub 2013 Feb 8.


The anticancer effect of phospho-tyrosol-indomethacin (MPI-621), a novel phosphoderivative of indomethacin: in vitro and in vivo studies.

Zhou D, Papayannis I, Mackenzie GG, Alston N, Ouyang N, Huang L, Nie T, Wong CC, Rigas B.

Carcinogenesis. 2013 Apr;34(4):943-51. doi: 10.1093/carcin/bgs394. Epub 2013 Jan 21.


Platinum folate nanoparticles toxicity: cancer vs. normal cells.

Mironava T, Simon M, Rafailovich MH, Rigas B.

Toxicol In Vitro. 2013 Mar;27(2):882-9. doi: 10.1016/j.tiv.2013.01.005. Epub 2013 Jan 11.


Nanodelivery strategies in cancer chemotherapy: biological rationale and pharmaceutical perspectives.

Mattheolabakis G, Rigas B, Constantinides PP.

Nanomedicine (Lond). 2012 Oct;7(10):1577-90. doi: 10.2217/nnm.12.128. Review.


FT-IR microspectroscopy of mouse colon tissues: insight into the chemistry of carcinogenesis and diagnostic potential.

Cohenford MA, Lim S, Brown C, Chaudhry MA, Sigdel S, Beckelhimer E, Rigas B.

Am J Pathol. 2012 Dec;181(6):1961-8. doi: 10.1016/j.ajpath.2012.08.039. Epub 2012 Oct 10.


MC-12, an annexin A1-based peptide, is effective in the treatment of experimental colitis.

Ouyang N, Zhu C, Zhou D, Nie T, Go MF, Richards RJ, Rigas B.

PLoS One. 2012;7(7):e41585. doi: 10.1371/journal.pone.0041585. Epub 2012 Jul 23.


Topical phospho-sulindac (OXT-328) is effective in the treatment of non-melanoma skin cancer.

Cheng KW, Mattheolabakis G, Wong CC, Ouyang N, Huang L, Constantinides PP, Rigas B.

Int J Oncol. 2012 Oct;41(4):1199-203. doi: 10.3892/ijo.2012.1577. Epub 2012 Jul 27.


In vitro and in vivo metabolic studies of phospho-aspirin (MDC-22).

Xie G, Wong CC, Cheng KW, Huang L, Constantinides PP, Rigas B.

Pharm Res. 2012 Dec;29(12):3292-301. doi: 10.1007/s11095-012-0821-6. Epub 2012 Jul 11.


Phospho-sulindac (OXT-328) inhibits the growth of human lung cancer xenografts in mice: enhanced efficacy and mitochondria targeting by its formulation in solid lipid nanoparticles.

Zhu R, Cheng KW, Mackenzie G, Huang L, Sun Y, Xie G, Vrankova K, Constantinides PP, Rigas B.

Pharm Res. 2012 Nov;29(11):3090-101. doi: 10.1007/s11095-012-0801-x. Epub 2012 Jun 22.


Phosphosulindac (OXT-328) selectively targets breast cancer stem cells in vitro and in human breast cancer xenografts.

Zhu C, Cheng KW, Ouyang N, Huang L, Sun Y, Constantinides P, Rigas B.

Stem Cells. 2012 Oct;30(10):2065-75. doi: 10.1002/stem.1139.


Regioselective oxidation of phospho-NSAIDs by human cytochrome P450 and flavin monooxygenase isoforms: implications for their pharmacokinetic properties and safety.

Xie G, Wong CC, Cheng KW, Huang L, Constantinides PP, Rigas B.

Br J Pharmacol. 2012 Sep;167(1):222-32. doi: 10.1111/j.1476-5381.2012.01982.x.


Preclinical predictors of anticancer drug efficacy: critical assessment with emphasis on whether nanomolar potency should be required of candidate agents.

Wong CC, Cheng KW, Rigas B.

J Pharmacol Exp Ther. 2012 Jun;341(3):572-8. doi: 10.1124/jpet.112.191957. Epub 2012 Mar 23.


Phospho-ibuprofen (MDC-917) suppresses breast cancer growth: an effect controlled by the thioredoxin system.

Sun Y, Rowehl LM, Huang L, Mackenzie GG, Vrankova K, Komninou D, Rigas B.

Breast Cancer Res. 2012 Jan 31;14(1):R20.


Phospho-ibuprofen (MDC-917) incorporated in nanocarriers: anti-cancer activity in vitro and in vivo.

Nie T, Wong CC, Alston N, Aro P, Constantinides PP, Rigas B.

Br J Pharmacol. 2012 Jun;166(3):991-1001. doi: 10.1111/j.1476-5381.2011.01799.x.


Carboxylesterases 1 and 2 hydrolyze phospho-nonsteroidal anti-inflammatory drugs: relevance to their pharmacological activity.

Wong CC, Cheng KW, Xie G, Zhou D, Zhu CH, Constantinides PP, Rigas B.

J Pharmacol Exp Ther. 2012 Feb;340(2):422-32. doi: 10.1124/jpet.111.188508. Epub 2011 Nov 15.


Sterically stabilized liposomes incorporating the novel anticancer agent phospho-ibuprofen (MDC-917): preparation, characterization, and in vitro/in vivo evaluation.

Mattheolabakis G, Nie T, Constantinides PP, Rigas B.

Pharm Res. 2012 Jun;29(6):1435-43. doi: 10.1007/s11095-011-0619-y. Epub 2011 Nov 10.


Chemotherapeutic properties of phospho-nonsteroidal anti-inflammatory drugs, a new class of anticancer compounds.

Huang L, Mackenzie GG, Sun Y, Ouyang N, Xie G, Vrankova K, Komninou D, Rigas B.

Cancer Res. 2011 Dec 15;71(24):7617-27. doi: 10.1158/0008-5472.CAN-11-2349. Epub 2011 Oct 24.


The metabolism and pharmacokinetics of phospho-sulindac (OXT-328) and the effect of difluoromethylornithine.

Xie G, Nie T, Mackenzie GG, Sun Y, Huang L, Ouyang N, Alston N, Zhu C, Murray OT, Constantinides PP, Kopelovich L, Rigas B.

Br J Pharmacol. 2012 Apr;165(7):2152-66. doi: 10.1111/j.1476-5381.2011.01705.x.


Structure-activity relationship study of novel anticancer aspirin-based compounds.

Joseph S, Nie T, Huang L, Zhou H, Atmakur K, Gupta RC, Johnson F, Rigas B.

Mol Med Rep. 2011 Sep-Oct;4(5):891-9. doi: 10.3892/mmr.2011.534. Epub 2011 Jul 6.


Phospho-sulindac (OXT-328) combined with difluoromethylornithine prevents colon cancer in mice.

Mackenzie GG, Ouyang N, Xie G, Vrankova K, Huang L, Sun Y, Komninou D, Kopelovich L, Rigas B.

Cancer Prev Res (Phila). 2011 Jul;4(7):1052-60. doi: 10.1158/1940-6207.CAPR-11-0067. Epub 2011 Apr 4.

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