Oral Conventional Synthetic Disease-Modifying Antirheumatic Drugs with Antineoplastic Potential: a Review

Hsieh, Cho-Hsun; Huang, Yi-Wei; Tsai, Tsen‐Fang

doi:10.1007/s13555-022-00713-1

Cited by 4 publications

(3 citation statements)

References 165 publications

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“…4 Leflunomide acts by inhibiting the tyrosine kinase activity of growth factor receptors or mitochondrial enzymes, leading to the arrest of cell growth. 5 We think that the increase observed in tracer uptake in certain parts of the patient using leflunomide regularly during this period may have been caused by this drug. It may have influenced the yet unknown somatostatin receptor affinity, which may have led to this situation.…”

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confidence: 87%

“…Leflunomide is used in the treatment of rheumatoid arthritis and is also known as a steroid-sparing agent 4 . Leflunomide acts by inhibiting the tyrosine kinase activity of growth factor receptors or mitochondrial enzymes, leading to the arrest of cell growth 5 . We think that the increase observed in tracer uptake in certain parts of the patient using leflunomide regularly during this period may have been caused by this drug.…”

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confidence: 98%

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Effect of Leflunomide Use on 68Ga-DOTATATE Biodistribution in a Case With Neuroendocrine Tumor

et al. 2023

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A 58-year-old man who underwent surgery for a well-differentiated neuroendocrine tumor of pancreatic origin was evaluated with 68 Ga-DOTATATE PET/CT imaging in the follow-up period. After PET/CT findings consistent with disease remission, the patient was started on leflunomide treatment with the diagnosis of rheumatoid arthritis. The patient received leflunomide for 6 months. Then, 68 Ga-DOTATATE PET/CT scan was repeated to evaluate the primary disease outcome. Besides the disease remission, we also observed alterations in DOTATATE uptakes of some tissues and organs. In this case, we present the changes in 68 Ga-DOTATATE PET/CT scan findings after leflunomide use.

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confidence: 87%

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confidence: 98%

Effect of Leflunomide Use on 68Ga-DOTATATE Biodistribution in a Case With Neuroendocrine Tumor

et al. 2023

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“…Leflunomide and its metabolite teriflunomide, which are oral inhibitors of DHODH, are approved for the treatment of rheumatoid arthritis and relapsing multiple sclerosis but have also been found to be beneficial in other autoimmune diseases such as myasthenia gravis or systemic lupus [ 5 , 6 , 7 ]. Recent studies also report a promising effect in the treatment of neoplasms as well as in viral infections such as COVID-19 [ 8 , 9 , 10 , 11 ].…”

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confidence: 99%

Safety and Tolerability of KIO-101 Eye Drops in Healthy Volunteers and Patients with Ocular Surface Disease—A Phase I Study

Schmidl,

Hommer,

Kallab

et al. 2024

Pharmaceutics

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Purpose: Inhibitors of dihydroorotate dehydrogenase (DHODH) have been found to be potent anti-inflammatory agents. Recently, a topical formulation (KIO-101 eye drops) of a DHODH inhibitor has been developed. The aim of the present study was to evaluate the safety and tolerability of KIO-101 eye drops in Healthy Volunteers (HVs) and patients with conjunctival hyperemia. Methods: The study was carried out in a double-masked, placebo-controlled, randomized, parallel-group design with two parts. In part I, HVs received single and multiple instillations (four times daily for 12 consecutive days) of KIO-101 eye drops in ascending doses of 0.05%, 0.15%, and 0.30%, respectively. Part II was conducted in patients with conjunctival hyperemia who received 0.15% KIO-101 eye drops twice daily for 12 consecutive days. Ophthalmic and systemic safety examinations were performed on all participants. In part II, ocular hyperemia grading and an ocular surface disease index (OSDI) questionnaire were performed. Results: 24 HVs participated in part I and 21 patients in part II. KIO-101 eye drops were well tolerated in all subjects. No serious adverse events (SAEs) occurred, and all AEs that were reported were transient and considered mild to moderate. In the highest dose cohort (0.30%), epistaxis occurred in two subjects after multiple instillations. In part II, after 12 days treatment with 0.15% KIO-101, conjunctival hyperemia decreased by −1.1 ± 0.27 points in the treatment and −0.6 ± 0.79 points in the placebo group (p = 0.0385). OSDI decreased from 47.9 ± 18.7 to 27.6 ± 19.13 points in the treatment group, while in the placebo group, a change from 41.3 ± 12.08 to 27.3 ± 18.63 points occurred. Conclusions: A 12-day treatment regimen with topical KIO-101 eye drops at low and mid doses was safe and well tolerated in both HVs and patients with conjunctival hyperemia. The obtained results point towards an early sign of reduction in conjunctival hyperemia.

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Impact of upadacitinib on the risk of digestive events in patients with rheumatoid arthritis: A systematic review and meta-analysis of randomized controlled trials

Liu-yan,

Kun,

Cheng

et al. 2023

Heliyon

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Oral Conventional Synthetic Disease-Modifying Antirheumatic Drugs with Antineoplastic Potential: a Review

Abstract: There is an increasing trend of malignancy worldwide. Disease-modifying antirheumatic drugs (DMARDs) are the cornerstones for the treatment of immune-mediated inflammatory diseases (IMIDs), but risk of malignancy is a major concern for patients receiving DMARDs.

Cited by 4 publications

References 165 publications

Effect of Leflunomide Use on 68Ga-DOTATATE Biodistribution in a Case With Neuroendocrine Tumor

Effect of Leflunomide Use on 68Ga-DOTATATE Biodistribution in a Case With Neuroendocrine Tumor

Safety and Tolerability of KIO-101 Eye Drops in Healthy Volunteers and Patients with Ocular Surface Disease—A Phase I Study

Impact of upadacitinib on the risk of digestive events in patients with rheumatoid arthritis: A systematic review and meta-analysis of randomized controlled trials

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