LNTH-1363S

LNTH-1363S (alias: RTX-1363S) is a trifunctional small molecule, comprising a FAP-binding ligand, a pharmacokinetics-modulating albumin-binding moiety, and a chelator for incorporation of radiometals.

General

Type : PET probe, Pyrrolidine, Quinoline, Cyanide, Carboxamide

Chemical_Nomenclature : (2S)-2-[[(2S)-6-[[2-[4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl]acetyl]amino]-2-[3-[2-[2-[2-[[2-[4-[[2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]carbamoyl]quinolin-7-yl]oxyacetyl]amino]ethoxy]ethoxy]ethoxy]propanoylamino]hexanoyl]amino]-6-(hexanoylamino)hexanoic acid

Canonical SMILES : CCCCCC(=O)NCCCC[C@@H](C(=O)O)NC(=O)[C@H](CCCCNC(=O)CN1CCN(CCN(CC1)CC(=O)O)CC(=O)O)NC(=O)CCOCCOCCOCCNC(=O)COC2=CC3=NC=CC(=C3C=C2)C(=O)NCC(=O)N4CCC[C@H]4C#N

InChI : InChI=1S\/C58H88N12O17\/c1-2-3-4-13-49(71)61-18-8-6-12-47(58(82)83)66-57(81)46(11-5-7-19-62-51(73)38-67-23-25-68(39-54(76)77)27-28-69(26-24-67)40-55(78)79)65-50(72)17-29-84-31-33-86-34-32-85-30-21-63-52(74)41-87-43-14-15-44-45(16-20-60-48(44)35-43)56(80)64-37-53(75)70-22-9-10-42(70)36-59\/h14-16,20,35,42,46-47H,2-13,17-19,21-34,37-41H2,1H3,(H,61,71)(H,62,73)(H,63,74)(H,64,80)(H,65,72)(H,66,81)(H,76,77)(H,78,79)(H,82,83)\/t42-,46-,47-\/m0\/s1

InChIKey : RKBZIJIVRMJSBY-JQDVYGSZSA-N

Other name(s) : RTX-1363S  ||  SCHEMBL27257914  ||  SCHEMBL30783471  ||  [68 Ga]Ga-LNTH-1363S  ||  64Cu-LNTH-1363S  ||  68Ga-RTX-1363S


MW : 1225.4

Formula : C58H88N12O17

CAS_number :

PubChem : 170747966

UniChem : RKBZIJIVRMJSBY-JQDVYGSZSA-N

Target

Families : LNTH-1363S ligand of proteins in family
DPP4N_Peptidase_S9

Protein :
human-FAP

References (5)

Title : Mass Dose Effects in FAP-Directed Imaging: Influence of Administered Dose of [(68)Ga]Ga-LNTH-1363S on Image Quality - Enke_2026_J.Nucl.Med__
Author(s) : Enke JS , Baessler J , Chand G , Glantschnig L , Bai B , Sjoestrand K , Trepel M , Orcutt K , Dreher N , Patt M , Dierks A , Lapa C
Ref : J Nucl Med , : , 2026
Abstract :
PubMedSearch : Enke_2026_J.Nucl.Med__
PubMedID: 41611478
Gene_locus related to this paper: human-FAP

Title : Comparison of (68)Ga-FAPI and (18)F-DOPA PET\/CT in patients with medullary thyroid cancer - Hescheler_2026_Front.Endocrinol.(Lausanne)_17_1824054
Author(s) : Hescheler DA , Atiyat D , Lorenz K , Heinzel A , Reschke P , Almaguel FG , Petersen M , Eppard E , Wybranska J , Wuestemann J , Kreissl MC
Ref : Front Endocrinol (Lausanne) , 17 :1824054 , 2026
Abstract :
PubMedSearch : Hescheler_2026_Front.Endocrinol.(Lausanne)_17_1824054
PubMedID: 42422425

Title : Biodistribution and Radiation Dosimetry for [(68)Ga]Ga-LNTH-1363S, a Probe Targeting Fibroblast Activation Protein alpha - Enke_2025_J.Nucl.Med_66_1284
Author(s) : Enke JS , Schuller BW , Glantschnig L , Kircher M , Bundschuh RA , Dierks A , Patt M , Fenn EJ , Rinscheid A , Pfob CH , Amor Coarasa A , Babich JW , Hesterman JY , Lapa C
Ref : J Nucl Med , 66 :1284 , 2025
Abstract :
PubMedSearch : Enke_2025_J.Nucl.Med_66_1284
PubMedID: 40533357
Gene_locus related to this paper: human-FAP

Title : Preclinical Evaluation of (64)Cu-LNTH-1363S to Detect Cardiac FAP-Positive Fibroblasts Using PET Imaging - Heo_2025_J.Nucl.Med__
Author(s) : Heo GS , Nai YH , Otaegui JR , Yang S , Luehmann HP , Yuan G , Onthank D , Ennis M , Brown J , Lavine KJ , Gropler RJ , Liu Y
Ref : J Nucl Med , : , 2025
Abstract :
PubMedSearch : Heo_2025_J.Nucl.Med__
PubMedID: 41381234
Gene_locus related to this paper: human-FAP

Title : First-in-human study of a high affinity FAP imaging agent [Cu-64]LNTH-1363S - Hesterman_2024_J.Nuc.Med_65_241693
Author(s) : Hesterman J , Hillier S , DiMagno S , Orcutt K , Amor A , Novicki A , Fenn E , Friebe M , Purohit A , Kouri S , Monks N , Kazerounian S , Tully K , Russell D , Fanchon L , Hoppin J , Babich J
Ref : Journal of Nuclear Medicine , 65 :241693 , 2024
Abstract :
PubMedSearch : Hesterman_2024_J.Nuc.Med_65_241693
PubMedID:
Gene_locus related to this paper: human-FAP