Preferred Label : Etirinotecan Pegol;
NCIt synonyms : PEG-Irinotecan; Pegylated Irinotecan NKTR 102;
NCIt definition : An extended-release (ER) formulation composed of irinotecan, which is a semisynthetic
derivative of camptothecin and a topoisomerase I-inhibitor prodrug, that is conjugated,
via a proprietary biodegradable ester-based linker, to polyethylene glycol (PEG),
with antineoplastic activity. Upon administration of etirinotecan pegol (EP), the
agent penetrates into the leaky tumor vasculature and accumulates in the tumor. The
linker slowly hydrolyzes and releases irinotecan, which leads to sustained exposure
of the tumor to irinotecan. In turn, irinotecan is converted to the biologically active
metabolite 7-ethyl-10-hydroxy-camptothecin (SN38) by a carboxylesterase. SN38 inhibits
topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and
DNA; this results in DNA breaks that inhibit DNA replication and trigger apoptosis.
Pegylation provides improved systemic exposure, increases drug penetration into tumors
and decreases drug clearance, thereby increasing the duration of therapeutic effects
while lowering the toxicity profile.;
UNII : LJ16641SFT;
CAS number : 848779-32-8; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 848779-32-8
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Drug name : Onzeald;
Molecule name : NKTR 102; NKTR-102;
Origin ID : C74069;
UMLS CUI : C3659087;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
