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CompletedNCT06089265KHKi in HFIUpdated Jan 24, 2024

Ketohexokinase Inhibition in Hereditary Fructose Intolerance

A Phase 2 interventional study of PF-06801591 in HFI, sponsored by Maastricht University Medical Center. Completed at 1 site in Netherlands. Open to participants aged 18 Years and older, including healthy volunteers. Per ClinicalTrials.gov, last updated 2024-01-24.

Sponsored by Maastricht University Medical Center · Phase 2, Interventional, and Treatment

Phase
Phase 2
Study type
Interventional
Enrollment
8
Allocation
Non-randomized
Ages
18 Years and older
Sex
All
01

Study summary

Hereditary fructose intolerance (HFI) is a rare inborn error of metabolism. Patients with HFI develop acute abdominal pain, nausea, vomiting, hypoglycemia and proximal tubular dysfunction upon consumption of a fructose containing food product. In rare cases, (prolonged) fructose consumption can even lead to liver and kidney failure. Patients with HFI are therefore treated with a lifelong fructose-restricted diet. Animal studies have shown that the clinical manifestations of HFI are abrogated upon inhibition of ketohexokinase (KHK), the enzyme that catalyses the first step in fructose metabolism.

Recently, PF-06835919, a KHK inhibitor (KHKi), was developed as a new treatment for non-alcoholic fatty liver disease. The compound was well tolerated in several phase II clinical trials.

It is hypothesized that PF-06835919 is also effective in patients with HFI.

Read the detailed description

Rationale: Hereditary fructose intolerance (HFI) is a rare inborn error of metabolism. Patients with HFI develop acute abdominal pain, nausea, vomiting, hypoglycemia and proximal tubular dysfunction upon consumption of a fructose containing food product. In rare cases, (prolonged) fructose consumption can even lead to liver and kidney failure. Patients with HFI are therefore treated with a lifelong fructose-restricted diet. Animal studies have shown that the clinical manifestations of HFI are abrogated upon inhibition of ketohexokinase (KHK), the enzyme that catalyses the first step in fructose metabolism.

Recently, PF-06835919, a KHK inhibitor (KHKi), was developed as a new treatment for non-alcoholic fatty liver disease. The compound was well tolerated in several phase II clinical trials.

It is hypothesized that PF-06835919 is also effective in patients with HFI. Objective: To study the effects of PF-06835919 on fructose tolerance and intrahepatic lipid content in patients with HFI. Study design: open-label, pilot study Study population: three adult patients with HFI will be treated with PF-06835919. Five adult healthy individuals will be included (but not be treated) as a reference. Intervention (if applicable): Patients receive once daily (in the morning) three tablets of 100 mg PF-06835919 for 9 days. They will subsequently be gradually exposed to increasing doses of either oral fructose or glucose (in a blinded fashion). Healthy individuals will only undergo oral fructose exposure, as a reference. Main study parameters/endpoints: Intrahepatic lipid content assessed by proton magnetic resonance spectroscopy (at baseline and completion), intestinal fructose tolerance (after oral fructose in comparison to oral glucose), hepatic fructose tolerance (serum glucose and phosphate after oral fructose in comparison to healthy individuals) and renal fructose tolerance (urinary glucose, phosphate, pH and amino acids after oral fructose in comparison to healthy individuals). Nature and extent

02

Conditions studied

  • HFI
03

Who can participate

Ages eligible
18 Years and older
Sexes eligible
All
Accepts healthy volunteers
Yes

Eligibility criteria

Inclusion Criteria:

  • Participants are able to provide signed and dated written informed consent prior to any study specific procedures
  • Use of effective contraception (only applicable to premenopausal women; a pregnancy test will be performed in these women at baseline)
  • Aged ≥ 18 years

Exclusion Criteria:

  • Diabetes mellitus
  • Pregnancy
  • Patients with congestive heart failure and/or severe renal and or liver insufficiency
  • Uncontrolled hypertension
  • Previous enrolment in a clinical study with an investigational product during the last 3 months or as judged by the investigator which would possibly hamper our study results
  • Use of drugs that inhibit organic anion transporting polypeptide B1 (OATPB1) transporters (e.g. rifampicin, gemfibrozil, ciclosporine, erythromcyin and clarithromycin)*
  • Treatment with irinotecan* Any contra-indications for MRI scanning*
  • Subjects who do not want to be informed about unexpected medical findings

    • Exclusion criterion for HFI patients only.
04

Study design

Phase
Phase 2
Primary purpose
Treatment
Allocation
Non-randomized
Intervention model
Parallel assignment
Masking
None (open label)
Enrollment
8 participants (actual)

Study arms

  • Experimental
    HFI patients

    HFI participants will receive PF-06835919 for 9 days. Dosage; once daily 300 mg PF-06835919 in the form of 3 tablets, oral.

    Drug: PF-06801591

  • No intervention
    Healthy controls

    Healthy controls will receive no intervention, but a single fructose tolerance test.

Interventions

  • DrugPF-06801591

    Active ketohexokinase inhibitor

    Also known as: KHKi

05

What researchers measure

Primary outcomes

  1. Intestinal Fructose tolerance,

    a visual analog scale from 1-10 for abdominal pain will be used. Additional every 5 minutes the participant will be asked if he/she is nauseous, and more, less or similar nauseous as 5 minutes before.

    Time frame: 9 days

  2. Intestinal Fructose tolerance,

    Every 5 minutes the participant will be asked if he/she is nauseous, and more, less or similar nauseous as 5 minutes before.

    Time frame: 9 days

  3. Renal Fructose tolerance

    Urinary pH

    Time frame: 9 days

  4. Renal Fructose tolerance

    Glucose content, mmol/L

    Time frame: 9 days

  5. Renal Fructose tolerance

    Phosphate content mmol/L

    Time frame: 9 days

  6. Renal Fructose tolerance

    Amino acid content mmol/L

    Time frame: 9 days

  7. Hepatic fructose tolerance

    Serum glucose levels, mmol/L

    Time frame: 9 days

  8. Hepatic fructose tolerance

    Serum phosphate levels, mmol/L

    Time frame: 9 days

Secondary outcomes

  1. Intrahepatic lipid content

    measured using 1H-MRS at baseline and completion

    Time frame: 9 days

  2. Blood pressure

    measured at baseline and completion. Both systolic and diastolic pressure will be assessed

    Time frame: 9 days

  3. Glycosylated transferrin

    measured at baseline and completion.

    Time frame: 9 days

06

Study locations

1 site
  • Maastricht University Medical centre
    Maastricht, Limburg 6202AZ, Netherlands
07

References and documents

Individual participant data

Plan to share: No — Data can be obtained with the PI on request

No publications or documents are linked to this record.

08

Registry details

Key details

Study ID
NCT06089265
Lead sponsor
Maastricht University Medical Center
Collaborators
Pfizer
Responsible party
Sponsor
First posted
Oct 18, 2023
Start date
Jun 15, 2023
Primary completion
Nov 30, 2023
Completion
Nov 30, 2023
Last update
Jan 24, 2024

Study contacts

Patrick Schrauwen, PhD
principal investigator · Maastricht University

Oversight

Data monitoring committee
No
FDA-regulated drug
No
FDA-regulated device
No
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