Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD

Figures & data

Figure 1 Structure of roflumilast and its metabolic inactivation.

Table 1 Patient demographics in the large, randomized roflumilast treatment trials

	Rabe 2005^Citation62	Calverley 2007^Citation63	Calverley 2009^Citation65	Fabbri 2009^Citation68
				Salmeterol	Tiotropium
Number randomized	1411	1513	3096	933	743
Mean age (years)	64	65	64	65	64
% male	74	76	75	66	72
Smoking history (pack years)	43	44	48	43	43
Current smokers (%)	46	37	41	39	40
FEV1 prebronchodilator	1.4	1.0	1.0	1.4	1.5
FEV1 (% predicted)	54	37	33	52	53

Notes: Data include number of patients randomized in each trial, mean age in years of patients in each trial, percentage of male patients, average smoking history in pack years (one pack year = one pack/day for one year), percentage of current smokers, mean prebronchodilator FEV₁, and mean FEV₁ as a percentage of the predicted value.

Abbreviation: FEV₁, forced expiratory volume in one second.

Table 2 Patient outcomes in the roflumilast treatment trials

	Rabe 2005^Citation62 500 μg	Calverley 2007^Citation63	Calverley 2009^Citation65	Fabbri 2009^Citation68
				Salmeterol	Tiotropium
Pre-FEV1 (mL)	88	36	48	49	80
Post-FEV1 (mL)	97	39	55	60	81
SGRQ	–1.7	+0.3
Dropouts (%)	22/11	29/22	33/31	23/18	17/10
Exacerbation rate	0.28/0.30	0.86/0.92	1.14/1.37	18/11	11/16
Weight loss (kg)	N/A	N/A	2.2	2.2	2.1
Diarrhea (%)	9/2	9/3	8/3	8/3	9/1
Nausea (%)	5/1	5/1	4/2	5/1	3/1
Headache (%)	N/A	6/2	3/1	3/1	2/0

Notes: Pre-FEV₁ refers to mean change in prebronchodilator FEV₁ at the end of the trial. Post-FEV₁ refers to the mean change in postbronchodilator FEV₁ at the end of the trial. SGRQ refers to change in mean St George Respiratory Question Score at the end of the treatment period. A reduction in score represents an improvement. Dropouts represent the percentage of patients that did not complete the treatment period. For each study, the first percentage represents the percentage of subjects in the roflumilast treatment arm that did not complete the study and the second percentage represents dropouts in the placebo arm. In each study, a greater percentage dropped out of the roflumilast treatment arms. The exacerbation rate refers to the number of moderate and severe exacerbations, exacerbation rate per patient, or the percentage of patients experiencing exacerbations during the study. In each case, the first number represents the roflumilast arm and the second the placebo arm of the studies. The next row contains the average difference in weight loss between the placebo arm and the treatment arms. In the three studies reporting weight loss, patients receiving roflumilast lost an average of slightly more than 2 kg more than the placebo-treated patients (N/A, data are not available). The last three rows represent the percentages of patients reporting diarrhea, nausea, and headache. In each case, the first percentage represents the percentage of patients reporting the side effect in the roflumilast arm and the second represents the percentage reporting the side effect in the placebo arm.

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