The purpose of this study is to investigate how safe the new compound ASTX660 is and how well it is tolerated when it is administered to healthy volunteers. ASTX660 has been administered to humans before. It has also been previously tested in the…
ID
Source
Brief title
Condition
- Other condition
- Leukaemias
Synonym
Health condition
solid tumors, lymphoma
Research involving
Sponsors and support
Intervention
Outcome measures
Primary outcome
To identify and quantify the main excretion pathways of ASTX660, including the
mass balance of excretion in urine and feces.
Secondary outcome
To determine the oral absolute bioavailability (F) of ASTX660 after single dose
administration in the fasted condition.
To determine the fraction of ASTX660 dose absorbed (Fa).
To determine the PK of ASTX660 following oral and IV administration.
To determine the safety and tolerability of ASTX660 following oral and IV
administration.
To identify the metabolites of ASTX660 in plasma, urine, and feces, if
feasible.
Background summary
ASTX660 is a new compound that may eventually be used for the treatment of
patients with advanced solid tumors, lymphoma, and acute myeloid leukemia and
for whom standard life-prolonging measures are not available.
ASTX660 is in development and is not registered as a drug but has been given to
humans before.
Study objective
The purpose of this study is to investigate how safe the new compound ASTX660
is and how well it is tolerated when it is administered to healthy volunteers.
ASTX660 has been administered to humans before. It has also been previously
tested in the laboratory and on animals.
It will also be investigated how quickly and to what extent ASTX660 is absorbed
and eliminated from the body. ASTX660 will be labeled with 14 Carbon (14C) and
is thus radioactive. In this way ASTX660 can be traced in blood, urine and
feces. The additional radiation you will be exposed to in this study is
negligible.
Study design
The actual study will consist of 2 periods: the volunteer will stay in the
research center for 6 days (5 nights) (Period 1) and up to 11 days (10 nights)
(Period 2), with at least 4 days between the end of Period 1 and the start of
Period 2.
ASTX660 will be given as an oral capsule with 240 milliliters (mL) of tap water
and an intravenous infusion (solution of the compound that will be administered
directly in a blood vessel). On Day 1 in Period 1, 1 hour after receiving
ASTX660 as an oral capsule, the colunteer will receive 100 microgram (µg)
containing 14C-radiolabeled ASTX660 as an intravenous injection. On Day 1 in
Period 2, the volunteer will receive 120 mg ASTX660 containing 14C radiolabeled
ASTX660 as a single oral capsule.
During the first 4 hours after oral administration of the study compound the
volunteer is not be allowed to lie down (except when told you can by
responsible doctor or study staff), as this may influence the uptake of the
study compound.
The planned treatment for the study is as follows:
Day Study
Compounds
Formulation How often
Day 1, Period 1 ASTX660, 120
mg Oral
capsule Once
Day 1, Period 1 ASTX660, 100 µg containing 14C radiolabeled ASTX660
Intravenous solution, injection Once
Day 1, Period 2 ASTX660, 120 mg containing 14C radiolabeled ASTX660 Oral
capsule Once
Intervention
ASTX660 will be given as an oral capsule with 240 milliliters (mL) of tap water
and an intravenous infusion (solution of the compound that will be administered
directly in a blood vessel). On Day 1 in Period 1, 1 hour after receiving
ASTX660 as an oral capsule, the colunteer will receive 100 microgram (µg)
containing 14C-radiolabeled ASTX660 as an intravenous injection. On Day 1 in
Period 2, the volunteer will receive 120 mg ASTX660 containing 14C radiolabeled
ASTX660 as a single oral capsule.
Study burden and risks
The study compound may cause side effects.
ASTX660 has been administered to 152 patients with advanced solid tumors and
lymphomas. The following side effects were most frequently observed (in >=15% of
patients or more) in these patients:
• fatigue
• increased lipase level in the blood
• increased amylase level in the blood
• nausea
• diarrhea
• vomiting
• anemia
• skin rash / skin rash with spots and bumps
• constipation
• pruritus (itching)
• increased alanine aminotransferase level in the blood
• edema peripheral (fluid retention)
• cough
The study compound may also have side effects that are still unknown.
Possible discomforts due to procedures
Drawing blood and/or insertion of the indwelling cannula may be painful or
cause some bruising.
In total, we will take about 360 mL of blood from you. This amount does not
cause any problems in adults. To compare: a blood donation involves 500 mL of
blood being taken each time.
To make a heart tracing, electrodes will be pasted at specific locations on
your arms, chest and legs. Prolonged use of these electrodes can cause skin
irritation.
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, the volunteer may experience a stinging sensation and the
eyes may become watery.
Exposure to radiation
This study involves using radioactive markers. The additional radiation burden
in this study due to the administration of radiolabeled ASTX660 is study is
negligible.
If you participate in scientific research involving exposure to radiation more
often, you should discuss with the responsible doctor whether participation
would be safe.
Rosewood Drive Suite 200 4420
Pleasanton CA 94588
US
Rosewood Drive Suite 200 4420
Pleasanton CA 94588
US
Listed location countries
Age
Inclusion criteria
Gender: Male or female
Age: 18 to 65 years, inclusive, at screening
Body mass index: 18.0 to 30.0 kg/m2, inclusive at screening
Exclusion criteria
1. Employee of PRA or the Sponsor.
2. History of significant drug and/or food allergies.
3. Using alcohol in the 48 hours (2 days) prior to screening and each admission
to the clinical research center is not allowed.
4. Using tobacco products in the 3 months prior to screening.
5. Known significant mental illness or other condition, such as active alcohol,
or other substance abuse or addiction, that in the opinion of the Investigator
predisposes the subject to high risk of noncompliance with the protocol.
6. Positive drug and alcohol screen (opiates, methadone, cocaine, amphetamines
[including ecstasy], cannabinoids, barbiturates, benzodiazepines, tricyclic
antidepressants, and alcohol) at screening and each admission to the clinical
research center.
See the protocol for the complete overview
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 | EUCTR2020-000193-26-NL |
| CCMO | NL73633.056.20 |