US 12,115,256 B2
Targeted liposomal gemcitabine and methods thereof
Clet Niyikiza, Gulph Mills, PA (US); Victor Moyo, Ringoes, NJ (US); Zhenghong Xu, Arlington, MA (US); and Kaniz Khalifa, Billericsa, MA (US)
Assigned to L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
Filed by L.E.A.F. HOLDINGS GROUP LLC, Gulph Mills, PA (US)
Filed on Feb. 2, 2021, as Appl. No. 17/165,534.
Application 17/165,534 is a division of application No. 15/587,018, filed on May 4, 2017, granted, now 10,940,112.
Claims priority of provisional application 62/331,841, filed on May 4, 2016.
Prior Publication US 2021/0154140 A1, May 27, 2021
Int. Cl. A61K 9/127 (2006.01); A61K 31/337 (2006.01); A61K 31/4745 (2006.01); A61K 31/555 (2006.01); A61K 31/7068 (2006.01); A61K 31/716 (2006.01); A61K 33/243 (2019.01); A61K 45/06 (2006.01); A61K 47/68 (2017.01); A61K 47/69 (2017.01); A61P 31/18 (2006.01); A61P 35/00 (2006.01); C07K 16/28 (2006.01); C07K 16/30 (2006.01)
CPC A61K 9/1271 (2013.01) [A61K 31/337 (2013.01); A61K 31/4745 (2013.01); A61K 31/555 (2013.01); A61K 31/7068 (2013.01); A61K 33/243 (2019.01); A61K 45/06 (2013.01); A61K 47/6849 (2017.08); A61K 47/6851 (2017.08); A61K 47/6913 (2017.08); A61P 31/18 (2018.01); A61P 35/00 (2018.01); C07K 16/28 (2013.01); C07K 16/30 (2013.01); C07K 2317/24 (2013.01); C07K 2317/31 (2013.01); C07K 2317/569 (2013.01); C07K 2317/622 (2013.01); C07K 2317/92 (2013.01)] 24 Claims
 
1. A method of delivering gemcitabine to a tumor expressing a folate receptor on its surface, the method comprising the step of: administering a pharmaceutical composition comprising a targeted PEGylated liposomal gemcitabine (PLG) in an amount to deliver a therapeutically effective dose of the gemcitabine to the tumor, wherein the targeted PLG comprises: a unilamellar anionic PEGylated liposome encapsulating one or more agents, wherein the PEGylated liposome has a diameter in the range 80 nm to 130 nm wherein the one or more agents comprises gemcitabine and Beta 1, 6-glucan; wherein the PLG comprises one or more targeting moiety comprising an antibody, a fragment of an antibody or a component of an antibody having a specific affinity for at least one type of folate receptor, the one or more targeting moiety conjugated to one or more maleimide moieties attached to-one or both of a PEG and an exterior of the liposome.