Trial reportXenobiotica; the fate of foreign compounds in biological systems2011
Disposition, metabolism and mass balance of [(14)C]apremilast following oral administration.
Trial report in Xenobiotica; the fate of foreign compounds in biological systems, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to trial NCT05468346 (Clinical Trial of Absorption, Metabolism and Excretion of [14C]-HEC585 in Chinese Adult Male Healthy Subjects), which is not on this map. Cited by 18 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
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.
Clinical Trial of Absorption, Metabolism and Excretion of [14C]-HEC585 in Chinese Adult Male Healthy Subjects
Who cites it
18 citing papers in PubMed, 50 citations in OpenAlex.
- Pharmacokinetics and Bioequivalence of Apremilast Tablets in Chinese Healthy Subjects Under Fasting and Postprandial States.Drug design, development and therapy · 2024Trial
- Pharmacokinetics and tolerability of apremilast in healthy Korean adult men.Clinical and translational science · 2021Trial
- The effects of apremilast on the QTc interval in healthy male volunteers: a formal, thorough QT study.International journal of clinical pharmacology and therapeutics · 2016Trial
- The impact of co-administration of ketoconazole and rifampicin on the pharmacokinetics of apremilast in healthy volunteers.British journal of clinical pharmacology · 2014Trial
- Exploring the Therapeutic Landscape: A Narrative Review on Topical and Oral Phosphodiesterase-4 Inhibitors in Dermatology.Pharmaceutics · 2025Review
- Population pharmacokinetic and exposure-response analysis of apremilast in Japanese subjects with moderate to severe psoriasis.The Journal of dermatology · 2021Article
- Quantitation of Apremilast in Beagle Dogs Plasma by UPLC-MS-MS and Its Application to Pharmacokinetic Studies.Journal of analytical methods in chemistry · 2021Article
- Review
- Apremilast in the treatment of psoriatic arthritis: a perspective review.Therapeutic advances in musculoskeletal disease · 2017Review
- Apremilast, an oral phosphodiesterase 4 (PDE4) inhibitor: A novel treatment option for nurse practitioners treating patients with psoriatic disease.Journal of the American Association of Nurse Practitioners · 2016Article
- Impact of Renal Impairment on the Pharmacokinetics of Apremilast and Metabolite M12.Clinical pharmacology in drug development · 2016Article
- Apremilast (Otezla): A New Oral Treatment for Adults With Psoriasis and Psoriatic Arthritis.P & T : a peer-reviewed journal for formulary management · 2015Article
- Review
- The pharmacokinetic effect of coadministration of apremilast and methotrexate in individuals with rheumatoid arthritis and psoriatic arthritis.Clinical pharmacology in drug development · 2014Article
- Apremilast.Hospital pharmacy · 2014Article
- Apremilast: first global approval.Drugs · 2014Review
- Phosphodiesterase 4-targeted treatments for autoimmune diseases.BMC medicine · 2013Review
- Altered bone biology in psoriatic arthritis.Current rheumatology reports · 2012Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
12 authors at 4 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Apremilast is a novel, orally available small molecule that specifically inhibits PDE4 and thus modulates multiple pro- and anti-inflammatory mediators, and is currently under clinical development for the treatment of psoriasis and psoriatic arthritis. The pharmacokinetics and disposition of [(14)C]apremilast was investigated following a single oral dose (20 mg, 100 μCi) to healthy male subjects. Approximately 58% of the radioactive dose was excreted in urine, while faeces contained 39%. Mean C(max), AUC(0-∞) and t(max) values for apremilast in plasma were 333 ng/mL, 1970 ng*h/mL and 1.5 h. Apremilast was extensively metabolized via multiple pathways, with unchanged drug representing 45% of the circulating radioactivity and <7% of the excreted radioactivity. The predominant metabolite was O-desmethyl apremilast glucuronide, representing 39% of plasma radioactivity and 34% of excreted radioactivity. The only other radioactive components that represented >4% of the excreted radioactivity were O-demethylated apremilast and its hydrolysis product. Additional minor circulating and excreted compounds were formed via O-demethylation, O-deethylation, N-deacetylation, hydroxylation, glucuronidation and/or hydrolysis. The major metabolites were at least 50-fold less pharmacologically active than apremilast. Metabolic clearance of apremilast was the major route of elimination, while non-enzymatic hydrolysis and excretion of unchanged drug were involved to a lesser extent.
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What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.