Antiviral Efficacy of BILN 2061, A Novel Oral HCV Serine Protease Inhibitor, in

[Guest guest]

First Report on the Antiviral Efficacy of BILN 2061, A Novel Oral HCV Serine

Protease Inhibitor, in

Patients with Chronic Hepatitis C, Genotype 1 – abstract 866

Holger Hinrichsen, I Medizinische Universitatsklinik, Kiel, Germany; Yves

Benhamou, Groupe

Hospitalier Pitié-Salpetrière, Paris, France; Markus Reiser, Medizinische

Universitätsklinik,

Bochum, Germany; Roel Sentjens, Academic Medical Center, Amsterdam,

Netherlands; Hemer Wedemeyer,

Medizinische Hochschule, Hannover, Germany; L Calleja, Cimica Puerta de

Hierro, Madrid, Spain;

Xavier Forns, Hospital Clinico, Barcelona, Spain; Jens Crönlein, Gerhard

Nehmiz, Gerhard Steinmann,

Boehringer Ingelheim Pharma KG, Biberach, Germany

BILN 2061 is a potent and specific inhibitor of the HCV serine protease

in-vitro. In a first

exploratory trial in patients with minimal liver fibrosis, the effect of a

2-day oral treatment with

BILN 2061 on the HCV of genotype 1 was investigated.

In an open, sequential group comparison, 31 patients with HCV genotype 1

(InnoLiPA) and minimal

liver fibrosis (determined histologically) were treated with 25, 200 or 500

mg BILN 2061 twice daily

over 2 days, given orally as solution with PEG400. In each group, placebo

was randomized in the

ratio 2:8. Virus load (VL) was measured as HCV RNA by Cobas Amplicor HCV

Monitor v2.0.

Mean age of all 31 patients in the 3 groups (including over enrollment of 1

patient with 25mg) was

47± 10 years, 7/31 were female. 14/31 patients were naïve for anti-HCV

therapy. All patients

completed the study and were followed up for 10-14 days. Viral load

decreased by 1 LOG10 unit or

greater in 7/9, 8/8 and 8/8 patients, treated with 25, 200 and 500mg,

respectively, without

difference between naïve and pre-treated patients. No response was seen with

placebo.

After end of treatment, viral load returned to baseline levels within 1-7

days. Liver transaminases

did not increase during treatment. Vital signs, adverse events, routine

laboratory and ECG did not

show relevant drug- induced changes. Tolerability was rated “good” by the

investigators in all

cases.

The authors of this study concluded that BILN 2061, given p.o.(by mouth)

over 2 days at 25, 200 or

500mg twice a day, demonstrated antiviral activity against HCV genotype 1 in

patients with minimal

liver fibrosis. No safety issues were identified among the 25 patients

exposed to BILN 2061.

[Guest guest]

First Report on the Antiviral Efficacy of BILN 2061, A Novel Oral HCV Serine

Protease Inhibitor, in

Patients with Chronic Hepatitis C, Genotype 1 – abstract 866

Holger Hinrichsen, I Medizinische Universitatsklinik, Kiel, Germany; Yves

Benhamou, Groupe

Hospitalier Pitié-Salpetrière, Paris, France; Markus Reiser, Medizinische

Universitätsklinik,

Bochum, Germany; Roel Sentjens, Academic Medical Center, Amsterdam,

Netherlands; Hemer Wedemeyer,

Medizinische Hochschule, Hannover, Germany; L Calleja, Cimica Puerta de

Hierro, Madrid, Spain;

Xavier Forns, Hospital Clinico, Barcelona, Spain; Jens Crönlein, Gerhard

Nehmiz, Gerhard Steinmann,

Boehringer Ingelheim Pharma KG, Biberach, Germany

BILN 2061 is a potent and specific inhibitor of the HCV serine protease

in-vitro. In a first

exploratory trial in patients with minimal liver fibrosis, the effect of a

2-day oral treatment with

BILN 2061 on the HCV of genotype 1 was investigated.

In an open, sequential group comparison, 31 patients with HCV genotype 1

(InnoLiPA) and minimal

liver fibrosis (determined histologically) were treated with 25, 200 or 500

mg BILN 2061 twice daily

over 2 days, given orally as solution with PEG400. In each group, placebo

was randomized in the

ratio 2:8. Virus load (VL) was measured as HCV RNA by Cobas Amplicor HCV

Monitor v2.0.

Mean age of all 31 patients in the 3 groups (including over enrollment of 1

patient with 25mg) was

47± 10 years, 7/31 were female. 14/31 patients were naïve for anti-HCV

therapy. All patients

completed the study and were followed up for 10-14 days. Viral load

decreased by 1 LOG10 unit or

greater in 7/9, 8/8 and 8/8 patients, treated with 25, 200 and 500mg,

respectively, without

difference between naïve and pre-treated patients. No response was seen with

placebo.

After end of treatment, viral load returned to baseline levels within 1-7

days. Liver transaminases

did not increase during treatment. Vital signs, adverse events, routine

laboratory and ECG did not

show relevant drug- induced changes. Tolerability was rated “good” by the

investigators in all

cases.

The authors of this study concluded that BILN 2061, given p.o.(by mouth)

over 2 days at 25, 200 or

500mg twice a day, demonstrated antiviral activity against HCV genotype 1 in

patients with minimal

liver fibrosis. No safety issues were identified among the 25 patients

exposed to BILN 2061.

[Guest guest]

First Report on the Antiviral Efficacy of BILN 2061, A Novel Oral HCV Serine

Protease Inhibitor, in

Patients with Chronic Hepatitis C, Genotype 1 – abstract 866

Holger Hinrichsen, I Medizinische Universitatsklinik, Kiel, Germany; Yves

Benhamou, Groupe

Hospitalier Pitié-Salpetrière, Paris, France; Markus Reiser, Medizinische

Universitätsklinik,

Bochum, Germany; Roel Sentjens, Academic Medical Center, Amsterdam,

Netherlands; Hemer Wedemeyer,

Medizinische Hochschule, Hannover, Germany; L Calleja, Cimica Puerta de

Hierro, Madrid, Spain;

Xavier Forns, Hospital Clinico, Barcelona, Spain; Jens Crönlein, Gerhard

Nehmiz, Gerhard Steinmann,

Boehringer Ingelheim Pharma KG, Biberach, Germany

BILN 2061 is a potent and specific inhibitor of the HCV serine protease

in-vitro. In a first

exploratory trial in patients with minimal liver fibrosis, the effect of a

2-day oral treatment with

BILN 2061 on the HCV of genotype 1 was investigated.

In an open, sequential group comparison, 31 patients with HCV genotype 1

(InnoLiPA) and minimal

liver fibrosis (determined histologically) were treated with 25, 200 or 500

mg BILN 2061 twice daily

over 2 days, given orally as solution with PEG400. In each group, placebo

was randomized in the

ratio 2:8. Virus load (VL) was measured as HCV RNA by Cobas Amplicor HCV

Monitor v2.0.

Mean age of all 31 patients in the 3 groups (including over enrollment of 1

patient with 25mg) was

47± 10 years, 7/31 were female. 14/31 patients were naïve for anti-HCV

therapy. All patients

completed the study and were followed up for 10-14 days. Viral load

decreased by 1 LOG10 unit or

greater in 7/9, 8/8 and 8/8 patients, treated with 25, 200 and 500mg,

respectively, without

difference between naïve and pre-treated patients. No response was seen with

placebo.

After end of treatment, viral load returned to baseline levels within 1-7

days. Liver transaminases

did not increase during treatment. Vital signs, adverse events, routine

laboratory and ECG did not

show relevant drug- induced changes. Tolerability was rated “good” by the

investigators in all

cases.

The authors of this study concluded that BILN 2061, given p.o.(by mouth)

over 2 days at 25, 200 or

500mg twice a day, demonstrated antiviral activity against HCV genotype 1 in

patients with minimal

liver fibrosis. No safety issues were identified among the 25 patients

exposed to BILN 2061.

[Guest guest]

First Report on the Antiviral Efficacy of BILN 2061, A Novel Oral HCV Serine

Protease Inhibitor, in

Patients with Chronic Hepatitis C, Genotype 1 – abstract 866

Holger Hinrichsen, I Medizinische Universitatsklinik, Kiel, Germany; Yves

Benhamou, Groupe

Hospitalier Pitié-Salpetrière, Paris, France; Markus Reiser, Medizinische

Universitätsklinik,

Bochum, Germany; Roel Sentjens, Academic Medical Center, Amsterdam,

Netherlands; Hemer Wedemeyer,

Medizinische Hochschule, Hannover, Germany; L Calleja, Cimica Puerta de

Hierro, Madrid, Spain;

Xavier Forns, Hospital Clinico, Barcelona, Spain; Jens Crönlein, Gerhard

Nehmiz, Gerhard Steinmann,

Boehringer Ingelheim Pharma KG, Biberach, Germany

BILN 2061 is a potent and specific inhibitor of the HCV serine protease

in-vitro. In a first

exploratory trial in patients with minimal liver fibrosis, the effect of a

2-day oral treatment with

BILN 2061 on the HCV of genotype 1 was investigated.

In an open, sequential group comparison, 31 patients with HCV genotype 1

(InnoLiPA) and minimal

liver fibrosis (determined histologically) were treated with 25, 200 or 500

mg BILN 2061 twice daily

over 2 days, given orally as solution with PEG400. In each group, placebo

was randomized in the

ratio 2:8. Virus load (VL) was measured as HCV RNA by Cobas Amplicor HCV

Monitor v2.0.

Mean age of all 31 patients in the 3 groups (including over enrollment of 1

patient with 25mg) was

47± 10 years, 7/31 were female. 14/31 patients were naïve for anti-HCV

therapy. All patients

completed the study and were followed up for 10-14 days. Viral load

decreased by 1 LOG10 unit or

greater in 7/9, 8/8 and 8/8 patients, treated with 25, 200 and 500mg,

respectively, without

difference between naïve and pre-treated patients. No response was seen with

placebo.

After end of treatment, viral load returned to baseline levels within 1-7

days. Liver transaminases

did not increase during treatment. Vital signs, adverse events, routine

laboratory and ECG did not

show relevant drug- induced changes. Tolerability was rated “good” by the

investigators in all

cases.

The authors of this study concluded that BILN 2061, given p.o.(by mouth)

over 2 days at 25, 200 or

500mg twice a day, demonstrated antiviral activity against HCV genotype 1 in

patients with minimal

liver fibrosis. No safety issues were identified among the 25 patients

exposed to BILN 2061.