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A Double-blind Randomized, Placebo-Controlled Study and Open-label Long Term Extension to Evaluate the Efficacy and Safety of Elafibranor 80 mg in Patients with Primary Biliary Cholangitis with Inadequate Response or Intolerance to Ursodeoxycholic Acid

Phase 2/3
Active, not recruiting
Conditions
Primary Biliary Cholangitis
Interventions
Registration Number
2024-512232-30-00
Lead Sponsor
Ipsen Pharma
Brief Summary

To evaluate the effect of elafibranor (80 mg/day) on cholestasis as defined by the primary endpoint over 52 weeks of the treatment compared to placebo.

Detailed Description

Not available

Recruitment & Eligibility

Status
Ongoing, recruitment ended
Sex
Not specified
Target Recruitment
61
Inclusion Criteria

Must have provided written informed consent and agree to comply with the study protocol

Patients taking statins or ezetimibe must be on a stable dose for ≥ 2 months prior to screening

Females participating in this study must be of non-child bearing potential or must be using highly effective contraception for the full duration of the study and for 1 month after the last drug intake: •Non-child bearing potential: Cessation of menses for at least 12 months due to ovarian failure or surgical sterilization such as bilateral oophorectomy, or hysterectomy •Highly effective contraception methods include: a.Combined (estrogen and progrestogen containing) hormaonal contraception associated with inhibition of ovulation, oral, intravaginal or transdermal b.Progestogen-only hormonal contraception associated with inhibition of ovulation, oral, injectable or implantable c.Intrauterine device (IUD) d.Intrauterine hormoine release system (IUS) e.Bilateral tubal occlusion f.Vasectomized partner g.Sexual abstinence, if required by local IRB/IEC regulations and/or considered adequate by National laws (the reliability of sexual abstinence needs to be evaluated in relation to the duration of the clinical study and the preferred and usual lifestyle of the patient)

For patients who consent to have liver biopsy samples collected, patients in whom it is safe and practical to proceed with a liver biopsy, and who agree to have: a.1 liver biopsy during the Screening Period (if no historical biopsy within 6 months before screening is available) b.1 liver biopsy after 52-weeks of treatment

Males or females age of 18 to 75 years inclusive at first Screening Visit (SV)

PBC diagnosis as demonstrated by the presence of ≥ 2 of the following 3 diagnostic criteria: a. History of elevated ALP levels for ≥ 6 months prior to randomization (V1) b. Positive anti-mitochondrial antibodies (AMA) titers (> 1/40 on immunofluorescence or M2 positive by enzyme-linked immunosorbent assay [ELISA]) or positive PBC-specific antinuclear antibodies (ANA) c. Liver biopsy consistent with PBC

ALP ≥ 1.67x upper limit of normal (ULN)

Total bilirubin (TB) ≤ 2x ULN To ensure inclusion of a relevant ratio of patients with substantial risk of long-term clinical outcomes or moderate disease stage, approximately 10% of randomized patients will be moderately advanced per Rotterdam Criteria (TB > ULN or Albumin < lower limit of normal [LLN]) and approximately 20% will have a TB > 0.6 x ULN (patients at risk of progression)

Must have at least 4 available values for PBC Worst Itch Numeric Rating Scale (NRS) during each of the 7 day intervals in the 14 days prior to randomization (V1), for a total of at least 8 values for PBC Worst Itch NRS in the last 14 days prior to randomization (V1)

UDCA for at least 12 months (stable dose ≥ 3 months) prior to screening, or unable to tolerate UDCA treatment (no UDCA for ≥ 3 months) prior to screening (per country standard-of-care dosing)

If on colchicine must be on a stable dose for ≥ 3 months prior to screening

Medications for management of pruritus (e.g., cholestyramine, rifampin, naltrexone or sertraline) must be on a stable dose for ≥ 3 months prior to screening

Exclusion Criteria

History or presence of other concomitant liver disease including: a) Positive anti-hepatitis A virus (HAV) immunoglobulin M (IgM) antibodies or positive hepatitis B surface antigen (HBsAg) or positive anti-hepatitis C virus (HCV) ribonucleic acid (RNA) (tested for in case of known cured HCV infection or positive HCV Ab at screening) b) Primary sclerosing cholangitis (PSC) c) Alcoholic liver disease (ALD) d) Autoimmune hepatitis (AIH) or if treated for an overlap of PBC with AIH, or if there is suspicion and evidence of overlap AIH features, that cannot be explained alone by insufficient response to UDCA e) Nonalcoholic steatohepatitis (NASH) f)Gilbert's Syndrome (exclusion due to interpretability of bilirubin levels) g) Known history of alpha-1 antitrypsin deficiency

Patients with previous exposure to elafibranor

SV value ALT and/or AST > 5 x ULN

For patients with AT or TB>ULN at SV1, variability of AT or TB > 40%

SV value albumin<3.0 g/dl

Severely advanced patients according to Rotterdam criteria (TB > ULN and albumin < LLN)

SV value INR > 1.3 due to altered hepatic function

SV value CPK > 2 x ULN

Screening serum creatinine > 1.5 mg/dl

Significant renal disease, including nephritic syndrome, chronic kidney disease (defined as patients with markers of kidney failure damage or eGFR < 60 mL/min/1,73 m2) calculated by MDRD

Platelet count < 150 x 103/μL

Clinically significant hepatic decompensation, including: a) History of liver transplantation, current placement on a liver transplant list, current Model for End-Stage Liver Disease-Sodium (MELD-Na) score ≥ 12 linked to hepatic impairment b) Patients with cirrhosis/portal hypertension complications, including known esophageal varices, ascites, history of variceal bleeds or related interventions (e.g., insertion of variceal bands or transjugular intrahepatic portosystemic shunts [TIPS]), and hepatic encephalopathy, history or presence of spontaneous bacterial peritonitis, hepatocellular carcinoma c) Hepatorenal syndrome (type I or II)

AFP > 20 ng/mL with 4-phase liver CT or MRI imaging suggesting presence of liver cancer

Known hypersensitivity to the investigational product or to any of the formulation excipients of the elafibranor or placebo tablet

Mental instability or incompetence, such that the validity of informed consent or ability to be compliant with the study is uncertain

Medical conditions that may cause non-hepatic increases in ALP (e.g., Paget's disease) or which may diminish life expectancy to < 2 years, including known cancers

Patient has a positive test for Human Immunodeficiency Virus (HIV) Type 1 or 2 at screening, or patient is known to have tested positive for HIV

Evidence of any other unstable or untreated clinically significant immunological, endocrine, hematologic, gastrointestinal, neurological, or psychiatric disease as evaluated by the investigator; other clinically significant medical conditions that are not well controlled

History of alcohol abuse, defined as consumption of more than 30 g pure alcohol per day for men, and more than 20 g pure alcohol per day for women, or other substance abuse within 1 year prior to screening visit (SV1)

For female patients: known pregnancy, or has a positive serum pregnancy test, or lactating

Administration of the following medications are prohibited as specified below: a) 2 months prior to screening: fibrates and glitazones b) 3 months prior to screening: azathioprine, cyclosporine, methotrexate, mycophenolate, pentoxifylline, budesonide and other systemic corticosteroids (parenteral and oral chronic administration only); potentially hepatotoxic drugs (including α-methyl-dopa, sodium valproic acid isoniazid, or nitrofurantoin) c) 12 months prior to screening: antibodies or immunotherapy directed against ILs or other cytokines or chemokines d) For patients with previous exposure to OCA, OCA should be discontinued 3 months prior to screening

Patients who are currently participating in, plan to participate in, or have participated in an investigational drug study or medical device study containing active substance within 30 days or five half-lives, whichever is longer, prior to screening; for patients with previous exposure to seladelpar, seladelpar should be discontinued 3 months prior to screening

Study & Design

Study Type
Interventional clinical trial of medicinal product
Study Design
Not specified
Arm && Interventions
GroupInterventionDescription
elafibranorelafibranorParticipants receiving elafibranor
Primary Outcome Measures
NameTimeMethod
Response to treatment at week 52 defined as ALP < 1.67 x ULN and TB ≤ULN and ALP decrease ≥ 15%.

Response to treatment at week 52 defined as ALP < 1.67 x ULN and TB ≤ULN and ALP decrease ≥ 15%.

Secondary Outcome Measures
NameTimeMethod
PK assessments by GFT505 and GF1007 concentrations measurement in plasma

PK assessments by GFT505 and GF1007 concentrations measurement in plasma

Response to treatment based on ALP normalization at week 52.

Response to treatment based on ALP normalization at week 52.

Change in pruritus from baseline through week 52 based on PBC Worst Itch NRS in patients with baseline PBC Worst Itch NRS score ≥4.

Change in pruritus from baseline through week 52 based on PBC Worst Itch NRS in patients with baseline PBC Worst Itch NRS score ≥4.

Change in pruritus from baseline through week 24 based on PBC Worst Itch NRS in patients with baseline PBC Worst Itch NRS score ≥4

Change in pruritus from baseline through week 24 based on PBC Worst Itch NRS in patients with baseline PBC Worst Itch NRS score ≥4

Change from baseline in ALP at 4, 13, 26, 39 and 52 weeks

Change from baseline in ALP at 4, 13, 26, 39 and 52 weeks

ALP response defined as 10%, 20% and 40% ALP reduction from baseline at week 52

ALP response defined as 10%, 20% and 40% ALP reduction from baseline at week 52

Response to treatment at week 52 according to: a) ALP < 1.5 x ULN, ALP decrease ≥ 40% and TB ≤ ULN b) ALP < 3 x ULN, AST <2x ULN and TB < 1 mg/dL (Paris I) c) ALP ≤ 1.5 x ULN, AST ≤ 1.5x ULN and TB ≤ ULN (Paris II) d) TB response rate of 15% change e) Normalization of abnormal TB and/or albumin (Rotterdam) f) TB ≤ 0.6 x ULN

Response to treatment at week 52 according to: a) ALP < 1.5 x ULN, ALP decrease ≥ 40% and TB ≤ ULN b) ALP < 3 x ULN, AST <2x ULN and TB < 1 mg/dL (Paris I) c) ALP ≤ 1.5 x ULN, AST ≤ 1.5x ULN and TB ≤ ULN (Paris II) d) TB response rate of 15% change e) Normalization of abnormal TB and/or albumin (Rotterdam) f) TB ≤ 0.6 x ULN

Safety and tolerability as assessed by: a) SAE, AE, AESI, physical examination, vital signs, medical history, ECG b) Chemistry and hematology c) Liver markers d) Renal biomarkers (including urinalysis) e) Other biochemical safety markers

Safety and tolerability as assessed by: a) SAE, AE, AESI, physical examination, vital signs, medical history, ECG b) Chemistry and hematology c) Liver markers d) Renal biomarkers (including urinalysis) e) Other biochemical safety markers

Response to treatment at week 52 according to: g) ALP ≤ 1.67 x ULN and TB ≤ 1 mg/dL [1] h) No worsening of TB defined as level of TB at week 52 < ULN or no increase from baseline of more than 0.1XULN at week 52 i) Complete biochemical response defined as normal ALP; TB; AST; ALT; albumin; and INR

Response to treatment at week 52 according to: g) ALP ≤ 1.67 x ULN and TB ≤ 1 mg/dL [1] h) No worsening of TB defined as level of TB at week 52 < ULN or no increase from baseline of more than 0.1XULN at week 52 i) Complete biochemical response defined as normal ALP; TB; AST; ALT; albumin; and INR

PBC risk scores at week 52: UK PBC score [2] and GLOBE score [3]

PBC risk scores at week 52: UK PBC score [2] and GLOBE score [3]

Response based on the normalization of bilirubin at week 52

Response based on the normalization of bilirubin at week 52

Response based on the normalization of albumin at week 52

Response based on the normalization of albumin at week 52

Change from baseline to week 52 in hepatobiliary injury and liver function as measured by AST, ALT, GGT, 5' NT, total and conjugated bilirubin, albumin, INR and ALP fractionated (hepatic)

Change from baseline to week 52 in hepatobiliary injury and liver function as measured by AST, ALT, GGT, 5' NT, total and conjugated bilirubin, albumin, INR and ALP fractionated (hepatic)

Change from baseline to week 52 in biomarkers of inflammation as measured by hsCRP, fibrinogen, haptoglobin and TNF-α

Change from baseline to week 52 in biomarkers of inflammation as measured by hsCRP, fibrinogen, haptoglobin and TNF-α

Change from baseline to week 52 in immune response as measured by IgG and IgM

Change from baseline to week 52 in immune response as measured by IgG and IgM

Change from baseline to week 52 in biomarkers, and non-invasive measures of hepatic fibrosis as measured by ELF (HA, PIINP, TIMP-1), PAI-1, TGF-β, CK-18 (M65 and M30), Pro-C3 and liver stiffness measured by TE (continuous)

Change from baseline to week 52 in biomarkers, and non-invasive measures of hepatic fibrosis as measured by ELF (HA, PIINP, TIMP-1), PAI-1, TGF-β, CK-18 (M65 and M30), Pro-C3 and liver stiffness measured by TE (continuous)

Change from baseline to week 52 in lipid parameters as measured by TC, LDL-C, HDL-C, calculated VLDL-C and triglycerides (TG)

Change from baseline to week 52 in lipid parameters as measured by TC, LDL-C, HDL-C, calculated VLDL-C and triglycerides (TG)

Change from baseline to week 52 in FPG

Change from baseline to week 52 in FPG

Change from baseline to week 52 in bile acids and biomarkers of bile acid synthesis as measured by bile acids, C4 and FGF-19

Change from baseline to week 52 in bile acids and biomarkers of bile acid synthesis as measured by bile acids, C4 and FGF-19

Proportion of responders in PBC Worst Itch NRS according to clinically meaningful change; at least 30% reduction; and one point, two points or three points decrease in score from baseline through week 52 and through week 24 in patients with a baseline NRS score ≥ 4

Proportion of responders in PBC Worst Itch NRS according to clinically meaningful change; at least 30% reduction; and one point, two points or three points decrease in score from baseline through week 52 and through week 24 in patients with a baseline NRS score ≥ 4

Proportion of patients with no worsening of pruritus from baseline through week 52 and through week 24 as measured by the PBC Worst Itch NRS

Proportion of patients with no worsening of pruritus from baseline through week 52 and through week 24 as measured by the PBC Worst Itch NRS

Change from baseline to week 52 in 5D-Itch

Change from baseline to week 52 in 5D-Itch

Change from baseline to week 52 in PROMIS Fatigue Short Form 7a

Change from baseline to week 52 in PROMIS Fatigue Short Form 7a

Change from baseline to week 52 in ESS

Change from baseline to week 52 in ESS

Change from baseline to week 52 in PBC-40

Change from baseline to week 52 in PBC-40

Change from baseline to week 52 in health utility as measured by the EQ-5D-5L

Change from baseline to week 52 in health utility as measured by the EQ-5D-5L

Change from baseline to week 52 in serum markers of bone turnover and in bone mineral density (hip and lumbar) assessed by DEXA scanning

Change from baseline to week 52 in serum markers of bone turnover and in bone mineral density (hip and lumbar) assessed by DEXA scanning

Onset of clinical outcomes described as a composite endpoint composed of: a) MELD-Na >14 for patients with baseline MELD-Na <12 b) Liver transplant c) Uncontrolled ascites requiring treatment d) Hospitalization for new onset or recurrence of any of the following: i) variceal bleed ii) hepatic encephalopathy defined as West-Haven score of 2 or more iii) spontaneous bacterial peritonitis e) Death

Onset of clinical outcomes described as a composite endpoint composed of: a) MELD-Na >14 for patients with baseline MELD-Na <12 b) Liver transplant c) Uncontrolled ascites requiring treatment d) Hospitalization for new onset or recurrence of any of the following: i) variceal bleed ii) hepatic encephalopathy defined as West-Haven score of 2 or more iii) spontaneous bacterial peritonitis e) Death

Trial Locations

Locations (19)

Universitair Ziekenhuis Gent

🇧🇪

Gent, Belgium

Hopital Erasme

🇧🇪

Anderlecht, Belgium

Assistance Publique Hopitaux De Paris

🇫🇷

Paris, France

Centre Hospitalier Universitaire Reims

🇫🇷

Reims Cedex, France

Centre Hospitalier Universitaire Grenoble Alpes

🇫🇷

Grenoble Cedex 9, France

Gastroenterologie am Bayerischen Platz

🇩🇪

Berlin, Germany

Medizinische Hochschule Hannover

🇩🇪

Hanover, Germany

Universitaetsmedizin der Johannes Gutenberg-Universitaet Mainz KöR

🇩🇪

Mainz, Germany

Eugastro GmbH

🇩🇪

Leipzig, Germany

Goethe University Frankfurt

🇩🇪

Frankfurt Am Main, Germany

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Universitair Ziekenhuis Gent
🇧🇪Gent, Belgium
Xavier Verhelst
Site contact
+3293322371
xavier.verhelst@uzgent.be

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