US 11,957,760 B2
Folate receptor targeted nanoparticle drug conjugates and uses thereof
Kai Ma, Montgomery, NJ (US); Aranapakam M. Venkatesan, Rego Park, NY (US); Feng Chen, Princeton, NJ (US); Fei Wu, Plainsboro, NJ (US); Melik Ziya Türker, Princeton, NJ (US); Thomas Courtney Gardinier, II, Raritan, NJ (US); Geno J. Germano, Jr., Philadelphia, PA (US); Gregory Paul Adams, Hatboro, PA (US); and Francis Y. F. Lee, Yardley, PA (US)
Assigned to Elucida Oncology, Inc., Monmouth Junction, NJ (US)
Filed by Elucida Oncology, Inc., Monmouth Junction, NJ (US)
Filed on Mar. 14, 2023, as Appl. No. 18/183,328.
Application 18/183,328 is a division of application No. 17/867,025, filed on Jul. 18, 2022.
Application 17/867,025 is a continuation of application No. PCT/US2021/056610, filed on Oct. 26, 2021.
Claims priority of provisional application 63/254,837, filed on Oct. 12, 2021.
Claims priority of provisional application 63/242,201, filed on Sep. 9, 2021.
Claims priority of provisional application 63/222,181, filed on Jul. 15, 2021.
Claims priority of provisional application 63/155,043, filed on Mar. 1, 2021.
Claims priority of provisional application 63/117,110, filed on Nov. 23, 2020.
Claims priority of provisional application 63/116,393, filed on Nov. 20, 2020.
Claims priority of provisional application 63/105,995, filed on Oct. 27, 2020.
Prior Publication US 2023/0263899 A1, Aug. 24, 2023
Int. Cl. A61K 9/00 (2006.01); A61K 31/4192 (2006.01); A61K 47/10 (2017.01); A61K 47/54 (2017.01); A61K 47/55 (2017.01); A61K 47/60 (2017.01); A61K 47/69 (2017.01); A61K 49/00 (2006.01); A61P 35/00 (2006.01)
CPC A61K 47/552 (2017.08) [A61K 31/4192 (2013.01); A61K 47/10 (2013.01); A61K 47/545 (2017.08); A61K 47/551 (2017.08); A61K 47/558 (2017.08); A61K 47/60 (2017.08); A61K 47/6923 (2017.08); A61K 47/6929 (2017.08); A61K 49/0032 (2013.01); A61K 49/0093 (2013.01); A61P 35/00 (2018.01)] 30 Claims
OG exemplary drawing
 
1. A nanoparticle-drug conjugate (NDC) comprising:
(a) a silica nanoparticle;
(b) polyethylene glycol (PEG) that is covalently bonded to the surface of the silica nanoparticle;
(c) a targeting ligand comprising folic acid, wherein the targeting ligand is attached to the silica nanoparticle through a first spacer group; and
(d) a linker-payload conjugate, wherein:
(i) the payload is exatecan;
(ii) the linker-payload conjugate is attached to the silica nanoparticle through a second spacer group;
(iii) the linker is a protease-cleavable linker; and
(iv) the exatecan is released upon cleavage of the linker,
wherein the first spacer group and the second spacer group each comprise a structure of Formula (NP):

OG Complex Work Unit Chemistry
wherein
x is an integer of 0 to 20;
the silicon atom (Si) is a part of the silica nanoparticle; and
the custom character adjacent to the triazole moiety denotes a point of attachment to the targeting ligand or the linker-payload conjugate, either directly or indirectly.