Entocort EC (budesonide)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
General Information
Entocort EC has been approved by the FDA for the treatment of
mild-to-moderate, active Crohn's disease involving certain
sections of the small and large intestines (ileum and/or ascending
colon). This once-daily medication targets the intestines and is
then quickly metabolized, this reduces the amount of drug entering
the systemic circulation, potentially reducing side effects.
According to the Crohn's & Colitis Foundation of
America, there may be up to 1,000,000 Americans with inflammatory
bowel disease (IBD). The category of IBD includes both Crohn's
disease and ulcerative colitis, two similar disorders of unknown
origin. Crohn's disease typically occurs in the ileum and
colon, but it can take place in any section of the gastrointestinal
tract. Symptoms of the disorder can include diarrhea, crampy
abdominal pain, fever and sometimes bleeding from the rectum.
Clinical Results
Entocort EC was evaluated in five randomized, double-blind
trials that included 994 subjects with mild-to-moderate, active
Crohn's disease of the ileum and/or ascending colon. In these
studies, clinical improvement was defined as achievement of a
Crohn's Disease Activity Index (CDAI) score of less than or
equal to 150.
One of the trials was designed to compare treatment with
Entocort EC 9 mg every morning to a comparator. At baseline, the
median CDAI was 272. Entocort EC produced a 69% clinical
improvement rate after eight weeks of treatment compared to 45% for
the comparator.
Two of the trials were designed to compare Entocort EC to
treatment with a placebo. In the first trial, which included 258
subjects, increasing doses of Entocort EC (1.5 mg bid, 4.5 mg bid
or 7.5 mg bid) were evaluated. At baseline, the median CDAI was
290. Treatment with 9 mg per day produced statistically significant
results compared to placebo, and no additional benefit was seen
with an increased dose of 15 mg per day. In the second trial, the
median CDAI at baseline was 263. Neither 9 mg qd or 4.5 mg bid dose
levels produced statistically significant results compared to
placebo.
Two additional trials were designed to compare Entocort EC with
oral prednisolone. In the first trial, the clinical improvement
rates were equal (60%) between the Entocort EC 9 mg qd and
prednisolone groups. In the second trial, clinical response rates
were 52% for Entocort EC 9 mg qd and 65% for prednisolone. In both
trials, the proportion of subjects with normal plasma cortisol
values was significantly higher in the Entocort EC groups than in
the prednisolone groups at week eight.
Side Effects
The most common adverse events reported by subjects in Entocort
EC clinical trials include the following:
- Headache
- Respiratory infection
- Nausea
- Symptoms of hypercorticism
According to trial data, the frequency of
glucocorticosteroid-associated adverse events was substantially
reduced with Entocort EC capsules compared to prednisolone (at
equivalent doses).
Mechanism of Action
Budesonide has a high glucocorticoid effect and a weak
mineralocorticoid effect, and the affinity of budesonide to
glucocorticosteroid receptors, which reflects the intrinsic potency
of the drug, is about 200-fold that of cortisol and 15-fold that of
prednisolone.
Entocort EC contains granules that are coated to prevent
dissolution in gastric juice, but which dissolve at pH>5.5,
i.e., normally when the granules reach the duodenum. Thereafter, a
matrix of ethylcellulose with budesonide controls the release of
the drug into the intestinal lumen in a time-dependent manner.
(from Entocort EC Prescribing Information)
Additional Information
