The primary objective of this study is to obtain clinical proof of principle that the Addition of a PgP/BCRP inhibitor increases CNS concentrations of tyrosine kinase inhibitors by inhibition of drug efflux transporter function in the blood brain…
ID
Bron
Verkorte titel
Aandoening
Cancer
Brain metastases
Tyrosinse Kinase Inhibitors
Drug Transporters
Ondersteuning
Onderzoeksproduct en/of interventie
Uitkomstmaten
Primaire uitkomstmaten
Improved CNS penetration of 11C erlotinib after PGP/BCRP inhibitor administration.
Achtergrond van het onderzoek
The primary objective of this study is to obtain clinical proof of principle that the addition of a PgP/BCRP inhibitor
increases CNS concentrations of tyrosine kinase inhibitors by inhibition of drug efflux transporter function in the blood
brain barrier.
Every patient will undergo two PET scans. For both scans an intravenous bolus of [11C]erlotinib will be administered. For
the second scan patients will be instructed to take 1000 mg of a PGP/BCRP inhibitor orally. This will enable us to measure the uptake of [11C]erlotinib in the brain with and without PgP/BCRP inhibition.
Doel van het onderzoek
The primary objective of this study is to obtain clinical proof of principle that the Addition of a PgP/BCRP inhibitor
increases CNS concentrations of tyrosine kinase inhibitors by inhibition of drug efflux transporter function in the blood
brain barrier
Onderzoeksopzet
11C-erlotnib PET scan on 2 successive days.
Follow up visit 7+-2 days afterwards.
Onderzoeksproduct en/of interventie
- 2 11C-erlotinib PET scans. 1 with administration of a PGP/BCRP inhibitor and 1 without.
- 1 MRI of the brain.
Publiek
Department of Medical Oncology<br>
Plesmanlaan 121
N. Steeghs
Amsterdam 1066 CX
The Netherlands
+31 (0)20 5122570
n.steeghs@nki.nl
Wetenschappelijk
Department of Medical Oncology<br>
Plesmanlaan 121
N. Steeghs
Amsterdam 1066 CX
The Netherlands
+31 (0)20 5122570
n.steeghs@nki.nl
Belangrijkste voorwaarden om deel te mogen nemen (Inclusiecriteria)
The study population consists of cancer patients with advanced or metastatic solid tumors for whom no standard
therapy is available or for whom a TKI which is a PgP/BCRP substrate is a standard therapeutic option (erlotinib,
sunitinib, imatinib, gefitinib, sorafenib, lapatinib, crizotinib, vemurafenib).
Belangrijkste redenen om niet deel te kunnen nemen (Exclusiecriteria)
- Known brain metastases;
- Patients who have had previous treatment with central nervous system irradiation;
- Treatment with the tyrosine kinase inhibitor used as TKI PET tracer within three half lives before the PET scans;
- Patients with known alcoholism, drug addiction and/or psychiatric of physiological condition which in the opinion of
the investigator would impair study compliance;
- Patients are not allowed to use co-medication with PgP or BCRP modulators (including OTC medication)
- Patients are also not allowed to use co-medication which are PgP or BCRP substrates as this may lead to increased toxicity.
- Known hypersensitivity to erlotinib, elacridar or any excipients used in the formulation of either IMPs.
- Known contra-indications for a MRI scan.
Opzet
Deelname
Opgevolgd door onderstaande (mogelijk meer actuele) registratie
Geen registraties gevonden.
Andere (mogelijk minder actuele) registraties in dit register
Geen registraties gevonden.
In overige registers
| Register | ID |
|---|---|
| NTR-new | NL4629 |
| NTR-old | NTR4780 |
| Ander register | M14EEP : 2014-000281-21 |