OTEZLA TABLET STARTER PACK

Apremilast

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

Apremilast | Aprémilast | Apremilastum | N-{2-[(1S)-1-(3-Ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl}acetamide | Apremilast |

Description

Apremilast is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). It is indicated in the treatment of active psoriatic arthritis in adults (approved by the FDA in March 2014) and moderate to severe plaque psoriasis (approved by the FDA in September 2014). PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells. By inhibiting PDE-4, apremilast increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including PDE-4, TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase. By targeting a central component of the inflammatory signaling cascade rather than a single inflammatory marker, PDE-4 inhibition may restore the homeostatic balance between pro- and anti-inflammatory signalling.

Indication

Investigated for use/treatment in psoriasis and psoriatic disorders.

Mechanism of Action

Apremilast is a novel, orally available small molecule inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4). PDE-4 is a cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase that is predominantly located in inflammatory cells. By inhibiting PDE-4, apremilast increases intracellular levels of cAMP and thereby inhibits the production of multiple proinflammatory mediators including PDE-4, TNF-alpha, interleukin-2 (IL-2), interferon-gamma, leukotrienes, and nitric oxide synthase. By targeting a central component of the inflammatory signaling cascade rather than a single inflammatory marker, PDE-4 inhibition may restore the homeostatic balance between pro- and anti-inflammatory signalling.

Pharmacodynamics

Not Available

Pharmacokinetics

Absorption:

When taken orally, apremilast is absorbed with an absolute bioavailability of ~73%. Co-administration with food does not alter the extent of absorption.

Distribution:

Peak plasma concentrations (Cmax) occur at a median time (tmax) of ~2.5 hours.

Metabolism:

Apremilast is metabolized via multiple pathways, including cytochrome (CYP) 3A4-mediated oxidative metabolism with subsequent glucuronidation, non-enzymatic hydrolysis, and non-CYP3A4-mediated metabolism. The unchanged drug accounts for 45% of circulating radioactivity and <7 % of excreted radioactivity. The main metabolite of apremilast is O-desmethyl apremilast glucuronide (M12), with nine other minor metabolites all with at least 50-fold less potency than apremilast in inhibiting PDE-4 and TNF-a.

Elimination:

58% urine; 39% feces.

Half-life

6-9 hours.

Clearance

10 L/hr.

Toxicity

DEPRESSION AND SUICIDE: Apremilast has been associated with increased depression and suicidal behaviour in patients. WEIGHT LOSS: Apremilast has been associated with weight decrease in patients.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

OTEZLA TABLET STARTER PACK was registered with Health Science Authority of Singapore by CELGENE PTE LTD. It is marketed with the registration number of SIN15202P with effective from 2017-03-29.

This product contains 10mg of Apremilast in the form of TABLET, FILM-COATED.

The medicine was manufactured by Celgene International Sarl in SWITZERLAND, and Patheon Inc. in CANADA

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: L04AA32

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