Table 5.
Summary of the LEN-based patents/patent applications.
| Patent/Patent Application (Applicant; Filing Date) |
Summary |
|---|---|
| OBD-Listed Patents and Their Family Members | |
|
US9951043B2 (Gilead Sciences; 28 February 2014) |
This patent (priority application date of 1 March 2013) has an estimated expiry date of February 28, 2034, which may further be extended based on USFDA laws. This patent relates to therapeutic compounds for treating HIV infection and generically claims LEN and its pharmaceutically acceptable salts [51]. |
|
US10071985B2 (Gilead Sciences; 17 August 2017) |
This patent (priority application date of 19 August 2016) has an estimated expiry date of 17 August 2037, which may further be extended based on USFDA laws. This patent specifically claims LEN, its salts, pharmaceutical compositions, and amorphous solid form. This patent also exemplifies and provides the data of the antiviral assay in MT4 cells, cytotoxicity (EC50 and CC50), the pharmacokinetic study by IV route (Cmax, AUC, half-life, distribution, and clearance) in Sprague–Dawley rats, Beagle dogs, and Cynomologous monkey and the metabolic stability (cultured human liver hepatocytes) of LEN. The patent specifications state LEN is a potent antiviral compound with improved pharmacokinetic parameters [37]. |
|
US11267799B2 (Gilead Sciences; 16 August 2018) |
This patent (priority application date of 17 August 2017) has an estimated expiry date of 16 August 2038, which may further be extended based on USFDA laws. This patent claims crystalline Form I (the active ingredient of Sunlenca), Form II, and Form III of LEN sodium salt. It also claims the pharmaceutical composition of the claimed crystalline forms to treat/prevent HIV infection. Its specification also mentions amorphous and crystalline Form IV of LEN [52]. |
|
US10654827B2 (Gilead Sciences; 25 June 2018) |
This patent (priority application date of 19 August 2016; a family member of US10071985B2) has an estimated expiry date of 17 August 2037. This patent claims a method of treating HIV infection with LEN or its salts. It also claims treatment of HIV infection with a combination of LEN and existing HIV treatments (protease inhibitors, NRTIs, NNRTIs, integrase inhibitors, entry inhibitors, maturation inhibitors, and capsid inhibitors) and other therapies (immune-based therapies, PI3K inhibitors, HIV antibodies, HIV p17 matrix protein inhibitors, HIV vif gene modulators, HIV-1 viral infectivity factor inhibitors, HIV-1 Nef modulators, HIV-1 splicing inhibitors, HIV ribonuclease inhibitors, HIV GAG protein inhibitors, HIV POL protein inhibitors, reverse transcriptase priming complex inhibitors, HIV gene therapy, pharmacokinetic enhancers, and HIV vaccines). This patent specifically claims to treat HIV-1 infection with LEN in a combination of 4′-ethynyl-2-fluoro-2′-deoxyadenosine, bictegravir, tenofovir, or abacavir [53]. |
|
US2021009555A1 (Gilead Sciences; 26 May 2020) |
This patent application (Status: Notice of Allowance mailed) is a family member of US9951043B2 and claims a process for preparing LEN [54]. |
|
US2018273508A1 (Gilead Sciences; 2 March 2018) |
This patent application (Status: Abandoned) is a family member of US9951043B2 and claims a process for preparing LEN [55]. |
|
US2014303164A1 (Gilead Sciences; 28 February 2014) |
This patent application (Status: Abandoned) is a family member of US9951043B2 and claims LEN-related compounds [56]. |
|
US2020262815A1 (Gilead Sciences; 25 November 2019) |
This patent application (Status: Notice of Allowance mailed) is a family member of US10071985B2 and claims compounds that can be used to prepare LEN. |
|
US2022251069A1 (Gilead Sciences; 26 January 2022) |
This patent application (Status: Under examination) is a family member of US11267799B2 and claims the use of polymorphs of LEN in combination with other antivirals, including 4′-ethynyl-2-fluoro-2′-deoxyadenosine, bictegravir, tenofovir or abacavir to treat HIV infection [57]. |
|
US2020038389A1 (Gilead Sciences; 15 July 2019) |
A method of treating HIV-1 infection in a heavily treatment-experienced patient (e.g., patients with MDR HIV infection) with a therapeutically amount of LEN or its pharmaceutically acceptable salt alone or in combination with a protease inhibitor, NNRTI, NRTI, integrase inhibitor, and pharmacokinetic enhancers [36]. |
| Other important patents/applications of LEN | |
|
WO2022159877A1 (Brii Biosciences; 25 January 2022) |
A combination of capsid inhibitors (LEN) and an adenosine derivative (islatravir. an NRTI) for the treatment/prevention of HIV infection. This patent application is silent about the experimental details of the combination of LEN and islatravir [58]. |
|
WO2022155258A1 (Gilead Sciences; 12 January 2022) |
A vaccine for HIV-1 infection comprising polypeptide segments of one or more HIV-1 proteins that can be co-administered with anti-HIV agents, including capsid inhibitors (LEN, GS-CA1, AVI-621, AVI-101, AVI-201, and AVI-301). This patent application is silent about the experimental details of the combination of LEN and the claimed vaccine [59]. |
|
WO2021236944A1 (Gilead Sciences; 20 May 2021) |
A method of treating/preventing HIV infection utilizing bictegravir (injection) alone or in combination with a capsid inhibitor (LEN. GS-CA1, AVI-621, AVI-101, AVI-201, and AVI-301) or other anti-HIV drugs. This patent application is silent about the experimental details of the combination of LEN and bictegravir [60]. |
|
KR20220112771A (Viiv Healthcare; 7 December 2020) |
A method of treating HIV infection with a combination of cabotegravir and a capsid inhibitor (LEN) or other anti-HIV agents. This patent application is silent about the experimental details of the combination of LEN and cabotegravir [61]. |
|
WO2021011891A1 (Gilead Sciences; 17 July 2020) |
A method of treating HIV infection with a long-acting pharmaceutical formulation of tenofovir alafenamide containing sucrose acetate isobutyrate, which may optionally contain a capsid inhibitor (LEN). This patent application is silent about the experimental details of the combination of LEN and tenofovir [62]. |
|
WO2020247933A2 (Univ Missouri; 8 June 2020) |
This patent application claims cyclic or linear peptides as HIV-1 capsid inhibitors [63]. |