Trial reportBMC dermatology2015
Topical application of RTA 408 lotion activates Nrf2 in human skin and is well-tolerated by healthy human volunteers.
Trial report in BMC dermatology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT02029716 (A Phase 1 Study to Evaluate the Safety, Tolerability, Pharmacodynamics, and Pharmacokinetics of RTA 408 Lotion in Healthy Volunteers), which is not on this map. Cited by 20 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
A Phase 1 Study to Evaluate the Safety, Tolerability, Pharmacodynamics, and Pharmacokinetics of RTA 408 Lotion in Healthy Volunteers
Who cites it
20 citing papers in PubMed.
- Pharmacokinetics and pharmacodynamics of the novel Nrf2 activator omaveloxolone in primates.Drug design, development and therapy · 2019Trial
- NRF2 as a Therapeutic Target in Dermatological Disorders: Mechanisms and Molecules.Pharmaceuticals (Basel, Switzerland) · 2026Review
- RTA 408 attenuates TBHP-Induced apoptosis in nucleus pulposus cells via Nrf2/ARE and NF-κB signaling pathways: in vitro and in vivo evidence for mitigating rats' intervertebral disc degeneration.Arthritis research & therapy · 2025Article
- Radiation dermatitis in the hairless mouse model mimics human radiation dermatitis.Scientific reports · 2024Article
- Nrf2 Signaling Pathway: a Potential Therapeutic Target in Combating Oxidative Stress and Neurotoxicity in Chemotherapy-Induced Cognitive Impairment.Molecular neurobiology · 2024Review
- Impaired NRF2 Inhibits Recovery from Ischemic Reperfusion Injury in the Aging Kidney.Antioxidants (Basel, Switzerland) · 2023Article
- NRF2 in dermatological disorders: Pharmacological activation for protection against cutaneous photodamage and photodermatosis.Free radical biology & medicine · 2022Review
- Targeted de-repression of neuronal Nrf2 inhibits α-synuclein accumulation.Cell death & disease · 2021Article
- Nrf2 Activation Attenuates Chronic Constriction Injury-Induced Neuropathic Pain via Induction of PGC-1Oxidative medicine and cellular longevity · 2021Article
- Antioxidant Therapy and Antioxidant-Related Bionanomaterials in Diabetic Wound Healing.Frontiers in bioengineering and biotechnology · 2021Review
- Protective Role of Nrf2 in Renal Disease.Antioxidants (Basel, Switzerland) · 2020Review
- Genetic activation of Nrf2 reduces cutaneous symptoms in a murine model of Netherton syndrome.Disease models & mechanisms · 2020Article
- Review
- RTA 408 Inhibits Interleukin-1β-Induced MMP-9 Expression via Suppressing Protein Kinase-Dependent NF-κB and AP-1 Activation in Rat Brain Astrocytes.International journal of molecular sciences · 2019Article
- Novel Nrf2-Inducer Prevents Mitochondrial Defects and Oxidative Stress in Friedreich's Ataxia Models.Frontiers in cellular neuroscience · 2018Article
- Targeting NRF2 for Improved Skin Barrier Function and Photoprotection: Focus on the Achiote-Derived Apocarotenoid Bixin.Nutrients · 2017Review
- Nrf2: a potential therapeutic target for diabetic neuropathy.Inflammopharmacology · 2017Review
- RTA-408 Protects Kidney from Ischemia-Reperfusion Injury in Mice via Activating Nrf2 and Downstream GSH Biosynthesis Gene.Oxidative medicine and cellular longevity · 2017Article
- Safety, pharmacokinetics, and pharmacodynamics of oral omaveloxolone (RTA 408), a synthetic triterpenoid, in a first-in-human trial of patients with advanced solid tumors.OncoTargets and therapy · 2017Article
- NRF2-targeted therapeutics: New targets and modes of NRF2 regulation.Current opinion in toxicology · 2016Article
Corrections and comments
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundTopical application of the synthetic triterpenoid RTA 408 to rodents elicits a potent dermal cytoprotective phenotype through activation of the transcription factor Nrf2. Therefore, studies were conducted to investigate if such cytoprotective properties translate to human dermal cells, and a topical lotion formulation was developed and evaluated clinically.
methodsIn vitro, RTA 408 (3-1000 nM) was incubated with primary human keratinocytes for 16 h. Ex vivo, RTA 408 (0.03, 0.3, or 3 %) was applied to healthy human skin explants twice daily for 3 days. A Phase 1 healthy volunteer clinical study with RTA 408 Lotion (NCT02029716) consisted of 3 sequential parts. In Part A, RTA 408 Lotion (0.5 %, 1 %, and 3 %) and lotion vehicle were applied to individual 4-cm(2) sites twice daily for 14 days. In Parts B and C, separate groups of subjects had 3 % RTA 408 Lotion applied twice daily to a 100-cm(2) site for 14 days or a 500-cm(2) site for 28 days.
resultsRTA 408 was well-tolerated in both in vitro and ex vivo settings up to the highest concentrations tested. Further, RTA 408 significantly and dose-dependently induced a variety of Nrf2 target genes. Clinically, RTA 408 Lotion was also well-tolerated up to the highest concentration, largest surface area, and longest duration tested. Moreover, significant increases in expression of the prototypical Nrf2 target gene NQO1 were observed in skin biopsies, suggesting robust activation of the pharmacological target.
conclusionsOverall, these data suggest RTA 408 Lotion is well-tolerated, activates Nrf2 in human skin, and appears suitable for continued clinical development.
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