Pharmacological and toxicological effects of 6-hydroxy-2-mercaptopurine and 6-thioguanine in in vitro and in vivo models of arthritis by Nordin, Nurul Syuhada

“…The thiopurines include 6-mercaptopurine (6-MP), 6-hydroxy-2-mercaptopurine (6H2MP) and 6-thioguanine (6TG) are the immunosuppressive agents used in the treatment of acute lymphoblastic leukaemia, autoimmune disorders and organ transplant recipients. …”
Get full text

Case report: Dupilumab treatment improved type 2 disorders in a patient with IPEX syndrome diagnosis by C. Caruso, L. Laterza, C. R. Settanni, S. Colantuono, C. Di Mario, B. Tolusso, F. Castrì, E. Gremese, E. Gremese, F. Scaldaferri, F. Scaldaferri, A. Armuzzi, A. Armuzzi, C. De Simone, K. Peris, A. Chiricozzi, A. Gasbarrini, A. Gasbarrini, A. Gasbarrini

“…In consideration of the poor response to conventional immunosuppressants and the presence of type 2 inflammatory manifestations, treatment with dupilumab at an initial dose of 600 mg, followed by a maintenance dose of 300 mg every other week, according to atopic dermatitis labeled dose, was started and combined to oral budesonide 6 mg/day and 6-mercaptopurine 75 mg/day. The patient experienced a rapid improvement in bowel and skin symptoms, leading to a progressive tapering of steroids. …”
Get full text

Incidence of Myelotoxicity and Other Adverse Effects Related to Thiopurine Starting in Patients with Inflammatory Bowel Disease: Retrospective Observational Study in a Third-Level... by Gerard Grau, Eduard Brunet-Mas, Laura Patricia Llovet, Patricia Pedregal, Albert Villoria, Luigi Melcarne, Anna Puy, Belen Garcia-Sague, Luis Enrique Frisancho, María José Ramírez-Lázaro, Sergio Lario, Xavier Calvet

“…In 11 cases (11.2%), azathioprine (AZA) was switched to 6-mercaptopurine (6 MP) as 5 showed tolerance and 6 patients needed suspension due to AEs. …”
Get full text

ITPA polymorphisms do not predict additional risk beyond TPMT and NUDT15 for thiopurine-induced cytopenia in inflammatory bowel disease by A. Jena, N. Grover, P. Bhatia, M. Singh, D. Lad, K.K. Prasad, H. Singh, U. Dutta, V. Sharma

“…Material and methods: We enrolled consecutive IBD patients on thiopurines (azathioprine or 6-mercaptopurine) from January 2019–March 2020, at a tertiary care center in North India. …”
Get full text

Modulation of host glutamine anabolism enhances the sensitivity of small cell lung cancer to chemotherapy by Manabu Kodama, Gouji Toyokawa, Osamu Sugahara, Shigeaki Sugiyama, Naoki Haratake, Yuichi Yamada, Reona Wada, Shinkichi Takamori, Mototsugu Shimokawa, Tomoyoshi Takenaka, Tetsuzo Tagawa, Hiroki Kittaka, Takeshi Tsuruda, Kentaro Tanaka, Yushiro Komatsu, Keisuke Nakata, Yuri Imado, Koji Yamazaki, Isamu Okamoto, Yoshinao Oda, Masatomo Takahashi, Yoshihiro Izumi, Takeshi Bamba, Hideyuki Shimizu, Tomoharu Yoshizumi, Keiichi I. Nakayama

“…Inhibition of HPRT1 by 6-mercaptopurine (6-MP) in combination with methotrexate (MTX), which blocks the de novo purine synthesis pathway, attenuated the growth of SCLC in mouse xenograft models. …”
Get full text

Genome-Wide Methylation Profiling in 229 Patients With Crohn’s Disease Requiring Intestinal Resection: Epigenetic Analysis of the Trial of Prevention of Post-operative Crohn’s Dise... by Nicholas T. Ventham, Nicholas A. Kennedy, Rahul Kalla, Alex T. Adams, Alexandra Noble, Holly Ennis, Craig Mowat, Malcolm G. Dunlop, Jack Satsangi, Ian Arnott, Aiden Cahill, Malcolm Smith, Tariq Ahmad, Sreedhar Subramanian, Simon Travis, John Morris, John Hamlin, Anjan Dhar, Chuka Nwokolo, Cathryn Edwards, Tom Creed, Stuart Bloom, Mohamed Yousif, Linzi Thomas, Simon Campbell, Stephen J. Lewis, Shaji Sebastian, Sandip Sen, Simon Lal, Chris Hawkey, Charles Murray, Fraser Cummings, Jason Goh, James O. Lindsay, Naila Arebi, Lindsay Potts, Aileen J. McKinley, John M. Thomson, John A. Todd, Mhairi Collie, Ashley Mowat, Daniel R. Gaya, Jack Winter, Graham D. Naismith, Holly Ennis, Catriona Keerie, Steff Lewis, Robin J. Prescott, Gordan Lauc, Harry Campbell, Dermot P.B. McGovern, Vito Annese, Vlatka Zoldoš, Iain K. Permberton, Manfred Wuhrer, Daniel Kolarich, Daryl L. Fernandes, Evropi Theorodorou, Victoria Merrick Daniel I. Spencer, Richard A. Gardner, Ray Doran, Archana Shubhakar, Ray Boyapati, Igor Rudan, Paolo Lionetti, Irena Trbojević Akmačić, Jasminka Krištić, Frano Vuč ković, Jerko Štambuk, Mislav Novokmet, Maja Pučić-Baković, Olga Gornik, Angelo Andriulli, Laura Cantoro, Giancarlo Sturniolo, Gionata Fiorino, Natalia Manetti, Anna Latiano, Anna Kohn, Renata D’Inca`, Silvio Danese, Ian D. Arnott, Colin L. Noble, Charlie W. Lees, Alan G. Shand, Gwo-Tzer Ho, Lee Murphy, Jude Gibson, Louise Evenden, Nicola Wrobel, Tamara Gilchrist, Angie Fawkes, Guinevere S.M. Kammeijer, Florent Clerc, Noortje de Haan, Aleksandar Vojta, Ivana Samaržija, Dora Markulin, Marija Klasić, Paula Dobrinić, Yurii Aulchenko, Tim van den Heuve, Daisy Jonkers, Marieke Pierik

“…Methods: TOPPIC was a placebo-controlled, randomized controlled trial of 6-mercaptopurine at 29 UK centers in patients with CD undergoing ileocolic resection between 2008 and 2012. …”
Get full text

Tendencia epidemiológica de la enfermedad intestinal inflamatoria en pacientes pediátricos en América Latina: Grupo de Trabajo en Enfermedad Intestinal Inflamatoria, Sociedad Latin... by A. Larrosa-Haro, L. Abundis-Castro, M.B. Contreras, M.J. Gallo, L. Peña-Quintana, C.H. Targa Ferreira, P.A. Nacif, R. Vázquez-Frias, S. Bravo, A.B. Muñoz-Urribarri, M. Mejía-Castro, M. Orsi, J. Amil-Díaz, V. Busoni, J. Cohen-Sabban, F.J. Martin-Capri, R. Zablah, M.G. Rodríguez-Guerrero, V.L. Sdepanian

“…Drug regimens were limited to 5-aminosalicylic acid derivatives, azathioprine, 6-mercaptopurine, infliximab, and adalimumab. Conclusions: Pediatric inflammatory bowel disease in Latin America appears to have increased during the years included in the study period, with a predominance of moderate or severe ulcerative colitis. …”
Get full text

Effects of PRPS1 I72 mutations on drug resistance in acute lymphoblastic leukemia and its mechanisms by CUI Zhiyan, CHEN Yao, TAO Yue, SHEN Shuhong, LI Hui

“…Objective·To study whether mutations at the I72 site of phosphoribosyl pyrophosphate synthetase 1 (PRPS1) can induce resistance in acute lymphoblastic leukemia (ALL) cells to thiopurine chemotherapy drugs 6-mercaptopurine (6-MP) and 6-thioguanine (6-TG), and explain their mechanisms of action.Methods·The PRPS1 gene mutations (I72F, R177S and V316L) found in clinical practice and PRPS1 gene mutations (V208A and V289A) present in two ALL cell lines (KOPN72bi and RS4;11) were constructed into the vector pGV303 fused with green fluorescent protein (GFP), respectively. …”
Get full text

The Potential of Epigallocatechin-3-gallate (EGCG) as Complementary Medicine for the Treatment of Inflammatory Bowel Disease by Sabrina Schnur, Fabian Hans, Annika Dehne, Janina Osti, Malte-Ole Schneemann, Marc Schneider, Marius Hittinger

“…This corresponds to the immunosuppressant 6-Mercaptopurin and the biological drug Infliximab. The EGCG treatment significantly decreased the release of the pro-inflammatory cytokines IL-6 (to 0%) and IL-8 (to 14.2%), similar to the effect of the corticosteroid Prednisolone. …”
Get full text

Systemic Metabolomic Profiling of Acute Myeloid Leukemia Patients before and During Disease-Stabilizing Treatment Based on All-Trans Retinoic Acid, Valproic Acid, and Low-Dose Chem... by Ida Sofie Grønningsæter, Hanne Kristin Fredly, Bjørn Tore Gjertsen, Kimberley Joanne Hatfield, Øystein Bruserud

“…We performed untargeted serum metabolomic profiling for 44 AML patients receiving treatment based on ATRA and valproic acid combined with low-dose cytotoxic drugs (cytarabine, hydroxyurea, 6-mercaptopurin) which identified 886 metabolites. When comparing pretreatment samples from responders and non-responders, metabolites mainly belonging to amino acid and lipid (i.e., fatty acid) pathways were altered. …”
Get full text

Analysis of the NUDT15 gene and metabolites of azathioprine in Japanese patients with inflammatory bowel disease by Shizuka Suzuki, Kan Uchiyama, Yutaro Motoi, Yuuki Yoshii, Yukari Inoue, Takahiro Kubota, Shunichi Odahara, Yuichiro Ohtaki, Shinichiro Takami, Zensho Ito, Nobuhiro Sato, Toshifumi Ohkusa, Shigeo Koido, Masayuki Saruta

“…Methods To clarify the cause of thiopurine toxicity, we analysed nucleoside disphosphate-linked moiety X-type motif 15 (NUDT15) gene polymorphisms, i.e., R139C, V18I, and V19_V19insGV, and measured 6-mercaptopurines and 6-methylmercaptopurines (6-MMP) using the archived blood samples collected from 49 IBD patients for our previous study. …”
Get full text