The purpose of study Period 1 is to find out how much study compound, PF-07081532, is in your blood, urine, feces and exhaled air after you take a *radioactively-labeled" form of the study compound as a liquid that you drink. A radioactive…
ID
Source
Brief title
Condition
- Diabetic complications
Synonym
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
• To characterize the extent of excretion of total radioactivity in urine and
feces following administration of a single oral dose of [14C]PF-07081532.
• To characterize the metabolic profile and identify circulating and excreted
metabolites following administration of a single oral dose of
[14C]PF-07081532.
Secondary outcome
• To quantify plasma PK parameters of PF-07081532 and total radioactivity
following administration of a single oral dose of [14C]PF-07081532.
• To quantify plasma PK parameters of [14C]PF-07081532, following
administration of a single, IV, microdose of [14C]PF-07081532.
• To determine the absolute oral bioavailability (F) of PF-07081532 following
administration of a single oral dose of PF-07081532 compared to a single IV
microdose of [14C]PF-07081532.
• To determine the fraction of dose absorbed (Fa) following administration of a
single oral dose of [14C]PF-07081532.
• To evaluate safety and tolerability of PF-07081532, administered as a single
oral dose of [14C]PF-07081532 or a single oral dose of
PF-07081532 followed by administration of a single IV microdose of
[14C]PF-07081532.
Background summary
PF-07081532 is a new study compound which is being developed as a treatment
option for patients with type 2 diabetes, to lower blood sugar levels and for
the treatment of obesity, to lower body weight. Type 2 diabetes is a disease in
which a person*s body cannot make enough insulin (a hormone that helps control
the amount of glucose or sugar in the blood) or does not properly use the
insulin it makes; this can lead to too much sugar in the blood. Obesity is a
serious health condition characterized by excess weight or body fat that may
affect an individual*s health.
PF-07081532 acts like one of your naturally occurring hormones, called GLP-1,
or glucagon-like peptide 1. This hormone helps people feel full and helps to
lower blood sugar levels. Some medications that act this way are already
approved and being used to treat people living with diabetes or with obesity.
This study involves a new study compound, this means that it has not been
approved for use in this country and its use in this study is investigational
(experimental or being tested). This study is different from your regular
medical care. The purpose of regular medical care is to improve or otherwise
manage your health. The purpose of the research is to gather information to
advance science and medicine and does not replace your regular medical care.
Study objective
The purpose of study Period 1 is to find out how much study compound,
PF-07081532, is in your blood, urine, feces and exhaled air after you take a
*radioactively-labeled" form of the study compound as a liquid that you drink.
A radioactive label is a radioactive particle attached to a drug that lets
scientists measure the amount of study compound in your body over time.
The purpose of study Period 2 is to find out how well the study compound is
absorbed by the body. For this, you will take unlabeled study compound as a
liquid that you drink, and this will be compared to radio-labeled study
compound given directly in a vein.
The researchers will also be testing the safety of the study compound, and how
healthy people feel after taking a single dose.
PF-07081532 has been administered to humans before. In addition, it has been
tested in the laboratory and on animals.
Study design
The study lasts a maximum of 12 weeks from the inspection to the follow-up
check.
Period 1:
For Period 1, it is necessary that the volunteer stays in the research center
for at least 8 days (7 nights) and at most 22 days (21 nights). The duration of
the stay will depend on how quickly or slowly the radioactively-labeled study
compound leaves the body. There are criteria defined for this study, which the
study doctor will use to decide when the volunteer can leave the research
center. This may be as soon as Day 7, or he may need to stay until up to Day
21. The study team will be checking the levels of radioactively-labeled study
compound in the body frequently from Day 7 onward and we will let the volunteer
know as soon as possible if he has to stay longer or if the volunteer can go
home.
There must be at least 21 days between when the volunteer receives the dose of
study compound in Period 1 and in Period 2. If he has to stay until Day 21, it
may be decided that Period 2 starts immediately and the volunteer does not have
to go home between the periods. Please keep in mind that it is also possible
that there are multiple days between two periods, for example 14 days
Period 2:
For Period 2, it is necessary that the volunteers stays in the research center
for 8 days (7 nights). He will leave the research center on Day 7. This part of
the study has a different purpose, as described above, so the volunteer does
not have to stay in the research center for a maximum of 22 days as is the case
in period 1. However, if the study doctor believes it is necessary to protect
the health, the volunteer may be asked to remain in the clinic after Day 7.
Period 1 day 1:
The volunteer will be given the 14C radioactively-labeled study compound,
PF-07081532, as a drink of approximately 100 mL. After the volunteer drinks the
study compound, the cup will be rinsed 2 times with approximately 140 mL of
water, which he will also be required to drink to be sure that he has received
the full amount of the study compound.
Period 2 day 1:
The unlabelled study drug PF-07081532 is first given as a 100 ml drink. After
drinking the study drug, the cup is rinsed 2 times with approximately 140 ml of
water, which should also be drunk to ensure that the full amount of the study
drug has been received.
One hour after drinking the study drug dosing solution,
14C-radioactively-labeled study drug PF-07081532 is given as a solution to be
administered directly into a vein (an intravenous infusion). This will take
about 15 minutes.
Do not lie down for the first 4 hours after study drug administration (unless
instructed to do so by one of the study physicians), as this may affect how the
body absorbs the study drug.
Intervention
Period 1, Day 1, 30 milligram (mg) radioactively-labeled PF 07081532 in a 100
mL solution as a drink, once
Period 2, Day 1, 30 mg PF-07081532 in a 100 mL solution as a drink, once
Period 2, Day 1, 100 microgram (µg) radioactively-labeled PF-07081532 in a 10
mL solution, intravenous infusion, once over 15 minutes
Study burden and risks
Blood draw
Drawing blood may be painful or cause some bruising. The use of the indwelling
cannula can sometimes lead to inflammation, swelling, hardening of the vein,
blood clotting, and bleeding in the environment of the puncture site. In some
individuals, a blood draw can sometimes cause pallor, nausea, sweating, low
heart rate, or drop in blood pressure with dizziness or fainting.
In total, we will take about 500 milliliters of blood from screening to
follow-up. This amount does not cause any problems in adults. If the
investigator thinks it is necessary for the safety of a subject, extra samples
might be taken for possible additional testing. If this happens, the total
amount of blood drawn may be more than the amount indicated above.
Heart tracing
To make a heart tracing, electrodes will be placed on the arms, chest and legs.
Prolonged use of these electrodes can cause skin irritation.
Blood pressure
The test is usually painless, however as the blood pressure cuff squeezes the
arm while it inflates it may be uncomfortable. This feeling lasts only a few
seconds.
Demographic questions
Demographic questions ask for personal information, such as name, date of birth
and race. While collection of demographic information does not expose you to
physical risk, collection of such information may result in a loss of your
privacy if the information is lost or stolen.
Fasting
Fasting could cause dizziness, headache, stomach discomfort, or fainting.
Coronavirus test
Samples for the coronavirus test will be taken from the back of the nose and
throat using swabs. Taking the samples only takes a few seconds, but can cause
discomfort and can give an unpleasant feeling. Taking a sample from the back of
the throat may cause the volunteer to gag. When the sample is taken from the
back of the nose, they may experience a stinging sensation and their eyes may
become watery.
East 42 Street 235
New York CT 06320
US
East 42 Street 235
New York CT 06320
US
Listed location countries
Age
Inclusion criteria
1. Male participants must be 18 to 60 years of age, inclusive, at the time of
signing the ICF.
2. Male participants who are overtly healthy as determined by medical
evaluation including medical history, physical examination, blood pressure and
pulse rate measurement, standard 12-lead ECG, and laboratory tests.
3.BMI of 17.5 to 30.5 kg/m2; and a total body weight >50 kg (110 lb).
Exclusion criteria
1. Evidence or history of clinically significant hematological, renal,
endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric,
neurological, or allergic disease (including drug allergies, but excluding
untreated, asymptomatic, seasonal allergies at the time of dosing).
• Any condition possibly affecting drug absorption (eg, gastrectomy,
cholecystectomy).
• Positive testing at screening for HIV, HBsAg, HBcAb, HBsAb or HCVAb. Note: A
positive HBsAb due to hepatitis B vaccination is permissible.
2. Personal or family history of MTC or MEN2, or participants with suspected
MTC per the investigator*s judgement.
3. History of irregular bowel movements (eg, irritable bowel syndrome, frequent
episodes of diarrhea, or constipation defined by less than 1 bowel movement on
average per 2 days) or lactose intolerance.
Design
Recruitment
Followed up by the following (possibly more current) registration
No registrations found.
Other (possibly less up-to-date) registrations in this register
No registrations found.
In other registers
| Register | ID |
|---|---|
| EudraCT | EUCTR2022-003311-29-NL |
| CCMO | NL82970.056.22 |