#thiopurines
Looks like there is still a role for thiopurines in combo with VDZ in UC (VIEWS).

- VDZ levels are not affected by thiopurines
- may not be a good idea to stop thiopurines in:
--> histologically active disease
--> prior anti-TNF use

#IBDSky
November 22, 2024 at 11:23 AM
Time turns people into legends

1/🧵 on one of the most important women in med history: Gertrude B. Elion

You may not know her, but her discoveries changed medicine
She co-developed thiopurines (azathioprine, mercaptopurine), a breakthrough in immunosuppressive therapy, & won the Nobel Prize in 1988
March 8, 2025 at 3:08 PM
Our study on thiopurines and intrahepatic cholestasis of pregnancy (ICP) has just been published online!
journals.lww.com/ajg/abstract...

Excellent work by doctoral student Ngoc Nguyen! And a great collaboration including @arthurmageau.bsky.social , @rheumepi.bsky.social and others
Thiopurines and intrahepatic cholestasis of pregnancy in... : Official journal of the American College of Gastroenterology | ACG
based cohort study included all singleton pregnancies with prevalent SLE or IBD in Sweden, 2007-2022. Exposure was ≥1 dispensation for azathioprine or 6-mercaptopurine from last menstrual period date ...
journals.lww.com
July 24, 2025 at 5:38 AM
Jason Xu (@stjuderesearch.bsky.social) reports on impact of VNTR in TPMT promoter region (beyond coding variants in TPMT). Hypothesis: ↑ VNTR repeats associated w/ ↓ enzymatic activity of TPMT & ↑myelosuppression 2/2 thiopurines. Genotype pipeline below. Allele types vary w/ ancestry. (1/2) #ASH25
December 6, 2025 at 9:22 PM
1/ The toolkit behind the discovery is out.
In @natcomms.nature.com, we report the selective NUDT5 degrader toolkit that helped uncover NUDT5’s hidden biology - and show antagonistic roles for NUDT5 and NUDT15 in 6-TG response. doi.org/10.1038/s414...
Targeted Protein Degradation of NUDT5 Dissociates Catalytic Inhibition from Protein Loss in 6-Thioguanine Response - Nature Communications
Thiopurines are widely used drugs whose activity depends on cellular metabolism. Here, the authors develop chemical tools to remove NUDT5 and show that protein loss, but not inhibition, alters drug re...
doi.org
August 12, 2026 at 2:03 PM
#health #gerontology #womenshealth #primaryhealthcare #publichealth #menopause #NCDs

Immunosuppressants
(thiopurines, anti-TNF)
increase the risk of
lymphoma.

Combination therapy with
an immunosuppressant and an anti-TNF
conferred the highest risk (aOR 3.44).
.
academic.oup.com/ecco-jcc/art...
February 6, 2026 at 9:41 AM
Therapeutic drug monitoring
Usefulness of thiopurines therapeutic drug monitoring in patients with inflammatory bowel disease
#InflammatoryBowelDisease #TherapeuticDrugMonitoring #6thioguanineNucleotides #Drug #Pharmacokinetics
www.em-consulte.com/article/1735...
Usefulness of thiopurines therapeutic drug monitoring in patients with inflammatory bowel disease
Usefulness of thiopurines therapeutic drug monitoring in patients with inflammatory bowel disease
www.em-consulte.com
April 22, 2025 at 12:27 PM
✳️5, ✳️6, ✳️7. Immunomodulators 💊

❌ Thiopurines for induction

👍 Okay to use thiopurines for maintenance

❌ Methotrexate for induction or maintenance

6/9
November 19, 2024 at 9:32 PM
6/Thiopurines are salvaged to produce thiopurine nucleotides, which inhibit DNPB and incorporate into DNA, resulting in DNA damage and cell death. So a screen for suppressors of 6TG toxicity could identify genes required to activate salvage or suppress DNPB.
November 6, 2025 at 7:03 PM
Thiopurines and intrahepatic cholestasis of pregnancy.
MHRA Drug Safety Update
#pharmsky #medsky

www.gov.uk/drug-safety-...
Thiopurines and intrahepatic cholestasis of pregnancy
Intrahepatic cholestasis of pregnancy (ICP) has been rarely reported in patients treated with azathioprine products and is believed to be a risk applicable to all drugs in the thiopurine class (azathi...
www.gov.uk
May 16, 2025 at 6:36 PM
Also thanks to @ki.se, @scilifelab.se, @novonordisk.bsky.social, Cancerfonden, and Barncancerfonden for continued support.

#NUDT5 #metabolism #thiopurines #chemotherapy #cancer #biomarker #PROTACs #TPD

4/4
November 21, 2025 at 3:43 PM
16/TL/DR: The DNPB pathway has been known since the 1950s, and thiopurines have been used almost as long. NUDT5 regulates the activity of this pathway, and sensitivity to drugs that block it.
November 6, 2025 at 7:07 PM
My very talented PhD student Ngoc Nguyen will be presenting his poster on thiopurines and intrahepatic cholestasis of pregnancy at #ISPE tomorrow (Monday, 11:30 - 13:00, poster # B-277) stop by and say hi! He is a rising star in pharmaco- epidemiology 🌟🤩
August 17, 2025 at 3:20 PM
Happy to share a new preprint on NUDT5's role in regulating nucleoside analog (NA) drug efficacy. 🔗 👇

🧵: We show that perturbing NUDT5 abundance by RNAi or a PROTAC (DDD2), but not inhibition with TH5427, desensitizes cells to thiopurines and most NA drugs in a titratable manner.

1/n
NUDT5 regulates the global efficacy of nucleoside analog drugs by coordinating purine synthesis and PRPP allocation https://www.biorxiv.org/content/10.1101/2025.11.20.689348v1
November 21, 2025 at 3:43 PM
This weeks recommended paper is by Samuel Witus and Michael Rapé +team who show that purine nucleotides stabilise the PPAT–NUDT5 complex to provide feedback control of purine biosynthesis, while thiopurines exploit the same interface with greater potency: www.nature.com/articles/s41...
Metabolite glues as a means of purine sensing and chemotherapeutic response - Nature
Purines can act as endogenous molecular glues in human cells by anchoring a rate-limiting enzyme in purine biosynthesis to its inhibitor, and modifying this mechanism could provide a way to improve th...
www.nature.com
July 17, 2026 at 5:05 PM
Thiopurines have the most consistent malignancy associations in #IBD, with the strongest lymphoma signal observed with anti-TNF plus thiopurine therapy.

Read more: https://www.gastroenterologyadvisor.com/news/malignancy-risk-in-ibd-increased-with-thiopurine-and-or-anti-tnf-agent-use/
September 4, 2026 at 9:58 PM
The CPIC Pharmacogene Curation Expert Panel re-evaluated the star alleles of TPMT and NUDT15, two genes central to the metabolism of thiopurines used in cancer and autoimmune disease.

#pharmacogenomics #PGx #genomics
Clinical Functional Assignment of TPMT and NUDT15 Alleles by the Clinical Pharmacogenetics Implementation Consortium Pha
Thiopurine toxicity and dose adjustment · Clin Pharmacol Ther 2026
www.genox-veille.fr
August 17, 2026 at 10:47 AM
This weeks recommended paper is by Samuel Witus and Michael Rapé +team who show that purine nucleotides stabilise the PPAT–NUDT5 complex to provide feedback control of purine biosynthesis, while thiopurines exploit the same interface with greater potency: www.nature.com/articles/s41...
Metabolite glues as a means of purine sensing and chemotherapeutic response - Nature
Purines can act as endogenous molecular glues in human cells by anchoring a rate-limiting enzyme in purine biosynthesis to its inhibitor, and modifying this mechanism could provide a way to improve th...
www.nature.com
July 17, 2026 at 5:03 PM
An optimized LC-ESI-MS/MS assay for erythrocyte 6-TG and 6-MMPD: Addressing critical methodological considerations for thiopurine metabolite monitoring #JChromB www.sciencedirect.com/science/arti...
An optimized LC-ESI-MS/MS assay for erythrocyte 6-TG and 6-MMPD: Addressing critical methodological considerations for thiopurine metabolite monitoring
Thiopurines, a class of antimetabolites widely used in patients with inflammatory bowel disease (IBD) and acute lymphoblastic leukemia (ALL), are asso…
www.sciencedirect.com
November 26, 2025 at 6:55 PM
LC-MS/MS quantification of 6-methylthio-2′-deoxyguanosine and 6-thio-2′-deoxyguanosine in genomic DNA with enzymatically synthesized isotope-labelled internal standards #ABC link.springer.com/article/10.1...
LC-MS/MS quantification of 6-methylthio-2′-deoxyguanosine and 6-thio-2′-deoxyguanosine in genomic DNA with enzymatically synthesized isotope-labelled internal standards - Analytical and Bioanalytical ...
The thiopurines 6-mercaptopurine and 6-thioguanine (TG) are analogs of guanine and are used in the treatment of hematological malignancies and immune-mediated inflammatory diseases. The mechanism of a...
link.springer.com
November 23, 2025 at 1:57 PM
After reports of intrahepatic cholestasis of pregnancy after off-label use of thiopurines to treat inflammatory bowel disease in pregnant patients

FDA says it will require drugmakers to add new warnings about risk

www.fda.gov/drugs/drug-s...
April 29, 2024 at 5:45 PM
Risques de malformations congénitales majeures après exposition in utero aux thiopurines et aux anti-TNF en cas de maladie inflammatoire de l'intestin chez la mère sco.lt/5PEk6q
Risques de malformations congénitales majeures après exposition in utero aux thiopurines et aux anti-TNF en cas de maladie inflammatoire de l'intestin chez la mère | Life Sciences Université Paris-Sac...
Dans une étude publiée dans Clinical Gastroenterology and Hepatology, les médecins de gastroentérologie de l’hôpital Bicêtre-Paris-Saclay ont étudié le risque de malformations congénitales majeures (M...
sco.lt
March 11, 2025 at 9:14 PM