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PI3K/AKT signaling activation by roflumilast ameliorates rotenone-induced Parkinson's disease in rats.
Farid HA, Sayed RH, El-Shamarka ME, Abdel-Salam OME, El Sayed NS. Farid HA, et al. Inflammopharmacology. 2024 Apr;32(2):1421-1437. doi: 10.1007/s10787-023-01305-x. Epub 2023 Aug 4. Inflammopharmacology. 2024. PMID: 37541971 Free PMC article.
Furthermore, roflumilast has been proposed as a favorable candidate for the treatment of neurological disorders. The current study aimed to unravel the neuroprotective role of roflumilast in the rotenone model of PD in rats. Ninety male rats were allocated in …
Furthermore, roflumilast has been proposed as a favorable candidate for the treatment of neurological disorders. The current study ai …
Prediction of drug-drug interactions between roflumilast and CYP3A4/1A2 perpetrators using a physiologically-based pharmacokinetic (PBPK) approach.
Jia G, Ren C, Wang H, Fan C. Jia G, et al. BMC Pharmacol Toxicol. 2024 Jan 2;25(1):4. doi: 10.1186/s40360-023-00726-2. BMC Pharmacol Toxicol. 2024. PMID: 38167223 Free PMC article.
This study aimed to develop a physiologically-based pharmacokinetic (PBPK) model to predict changes in the pharmacokinetics (PK) and pharmacodynamics (PD, PDE4 inhibition) of roflumilast (ROF) and ROF N-oxide when co-administered with eight CYP3A4/1A2 perpetrators. …
This study aimed to develop a physiologically-based pharmacokinetic (PBPK) model to predict changes in the pharmacokinetics (PK) and pharmac …
Regulation of PD-L1 expression is a novel facet of cyclic-AMP-mediated immunosuppression.
Sasi B, Ethiraj P, Myers J, Lin AP, Jiang S, Qiu Z, Holder KN, Aguiar RCT. Sasi B, et al. Leukemia. 2021 Jul;35(7):1990-2001. doi: 10.1038/s41375-020-01105-0. Epub 2020 Dec 9. Leukemia. 2021. PMID: 33299141 Free PMC article.
Cyclic-AMP (cAMP) exerts suppressive effects in the innate and adaptive immune system. The PD-1/PD-L1 immune checkpoint downregulates T-cell activity. Here, we examined if these two immunosuppressive nodes intersect. ...This signaling axis is disarmed at two specifi …
Cyclic-AMP (cAMP) exerts suppressive effects in the innate and adaptive immune system. The PD-1/PD-L1 immune checkpoint downre …
Roflumilast escalates alpha-synuclein aggregate degradation in rotenone-induced Parkinson's disease in rats: Modulation of the ubiquitin-proteasome system and endoplasmic reticulum stress.
Desouky MA, George MY, Michel HE, Elsherbiny DA. Desouky MA, et al. Chem Biol Interact. 2023 Jul 1;379:110491. doi: 10.1016/j.cbi.2023.110491. Epub 2023 Apr 25. Chem Biol Interact. 2023. PMID: 37105514
Perturbation of the protein homeostasis circuit is one of the principal attributes associated with many neurodegenerative disorders, such as Parkinson's disease (PD). This study aimed to explore the neuroprotective effect of roflumilast (ROF), a phosphodiesterase-4 …
Perturbation of the protein homeostasis circuit is one of the principal attributes associated with many neurodegenerative disorders, such as …
Roflumilast-loaded nanostructured lipid carriers attenuate oxidative stress and neuroinflammation in Parkinson's disease model.
Roy D, Balasubramanian S, Kunte PP, Natarajan J, Sola P, Rymbai E, R PKM. Roy D, et al. J Drug Target. 2025 Jan;33(1):127-142. doi: 10.1080/1061186X.2024.2408724. Epub 2024 Oct 1. J Drug Target. 2025. PMID: 39316825
In our study, we aim to repurpose US FDA-approved PDE4 inhibitor for PD. Through in-silico study, we identified roflumilast (ROF) as the potential candidate targeting PDE4B2. In Drosophila PD expressing the A30P mutant alpha-synuclein model, ROF exhibited ant …
In our study, we aim to repurpose US FDA-approved PDE4 inhibitor for PD. Through in-silico study, we identified roflumilast (R …
Inhibition of phosphodiesterases 1 and 4 prevents myofibroblast transformation in Peyronie's disease.
Harding SL, Ilg MM, Bustin SA, Ralph DJ, Cellek S. Harding SL, et al. BJU Int. 2025 May;135(5):810-817. doi: 10.1111/bju.16631. Epub 2024 Dec 23. BJU Int. 2025. PMID: 39716367 Free PMC article.
Selective inhibitors of these enzymes prevented myofibroblast transformation in a concentration-dependent manner, with PDE1 inhibitor ITI-214 and PDE4 inhibitors roflumilast and roflumilast N-oxide showing greatest potency. ITI-214 and roflumilast N-oxide inc …
Selective inhibitors of these enzymes prevented myofibroblast transformation in a concentration-dependent manner, with PDE1 inhibitor ITI-21 …
p-CREB and p-DARPP-32 orchestrating the modulatory role of cAMP/PKA signaling pathway enhanced by Roflumilast in rotenone-induced Parkinson's disease in rats.
Essam RM, Kandil EA. Essam RM, et al. Chem Biol Interact. 2023 Feb 25;372:110366. doi: 10.1016/j.cbi.2023.110366. Epub 2023 Jan 24. Chem Biol Interact. 2023. PMID: 36706892
Thus, PDE4 inhibition could be a promising strategy for treating PD. Accordingly, the present study investigated the neuroprotective efficacy of roflumilast, a PDE4 inhibitor, in abolishing neurodegeneration in the rotenone-induced PD model. ...Therefore, the …
Thus, PDE4 inhibition could be a promising strategy for treating PD. Accordingly, the present study investigated the neuroprotective …
Roflumilast inhibits lipopolysaccharide-induced tumor necrosis factor-alpha and chemokine production by human lung parenchyma.
Buenestado A, Chaumais MC, Grassin-Delyle S, Risse PA, Naline E, Longchampt E, Tenor H, Devillier P. Buenestado A, et al. PLoS One. 2013 Sep 16;8(9):e74640. doi: 10.1371/journal.pone.0074640. eCollection 2013. PLoS One. 2013. PMID: 24066150 Free PMC article.
BACKGROUND: Roflumilast is the first phosphodiesterase-4 (PDE4) inhibitor to have been approved for the treatment of COPD. ...We also investigated roflumilast's interaction with the long-acting beta2-agonist formoterol. METHODS: Explants from 25 patients undergoing …
BACKGROUND: Roflumilast is the first phosphodiesterase-4 (PDE4) inhibitor to have been approved for the treatment of COPD. ...We also …
Clinical pharmacokinetics and pharmacodynamics of topical non-biological therapies for psoriasis patients.
Lo A, Greenzaid JD, Gantz HY, Chodri K, Feldman SR. Lo A, et al. Expert Opin Drug Metab Toxicol. 2024 Apr;20(4):235-248. doi: 10.1080/17425255.2024.2337749. Epub 2024 Apr 2. Expert Opin Drug Metab Toxicol. 2024. PMID: 38553411 Review.
AREAS COVERED: We conducted a literature review on the pharmacokinetic (PK) and pharmacodynamic (PD) properties of topical therapies for psoriasis. We discuss how the PK and PD characteristics of these therapies inform clinicians on efficacy and toxicity when prescr …
AREAS COVERED: We conducted a literature review on the pharmacokinetic (PK) and pharmacodynamic (PD) properties of topical therapies …
Phosphodiesterase-4 enzyme as a therapeutic target in neurological disorders.
Bhat A, Ray B, Mahalakshmi AM, Tuladhar S, Nandakumar DN, Srinivasan M, Essa MM, Chidambaram SB, Guillemin GJ, Sakharkar MK. Bhat A, et al. Pharmacol Res. 2020 Oct;160:105078. doi: 10.1016/j.phrs.2020.105078. Epub 2020 Jul 14. Pharmacol Res. 2020. PMID: 32673703 Review.
An inverse association between PDE4 and cAMP levels is the key mechanism in various pathophysiological conditions like airway inflammatory diseases-chronic obstruction pulmonary disease (COPD), asthma, psoriasis, rheumatoid arthritis, and neurological disorders etc. In 2011, r …
An inverse association between PDE4 and cAMP levels is the key mechanism in various pathophysiological conditions like airway inflammatory d …
16 results