Drug Repuposing Patents – What We Did Not Discuss

If you follow our discussions of patent documents claiming radically new uses for known compounds, published in the issues that ASSAY and Drug Development Technologies dedicates to drug repurposing, you might think that there is a lot of patenting activity going on in this field – indicative of broad commercial interest.

Actually, there is significantly more out there. However, the space we can allot to patents in these journal issues is limited, and even if that were not the case we cannot fill half of the issue with these discussions. And so we limit us to the most interesting examples, and try to cover the broadest therapeutic range that is achievable under these circumstances.

As an illustration, we have assembled the 14 PCT applications from Q1/17 that we identified but did NOT discuss, summarizing each in two or three sentences. (See here for the list of 11 documents from this 3-month period that we did discuss extensively, as published in Assay Drug Dev Technol. 2017; 15(3):127-32. doi: 10.1089/adt.2017.29057.pq1 [link]).


WO/2017/049036: Use of kinase inhibitors to manage tuberculosis and other infectious diseases
(Emory University, published March 23, 2017)
A combination therapy of imatinib (Novartis’ Glevec®/Gleevec®) and antibiotics decreases overall bacterial load. Mice infected with mycobacterium were administered 100 mg/kg/day alone, rifabtutin (2.5 mg/kg/day) alone, and/or a combination of both. CFU in the spleen were determined 7 days post-infection.

WO/2017/046357: Therapeutic uses of elsiglutide
(Helsinn Healthcare SA, published March 23, 2017)
Myelosuppression and immunocompromise caused by cytotoxic agents can be reversed by administering Helsinn’s GLP-2 analog elsiglutide (Phase II in chemotherapy-induced diarrhea completed in early 2016, no further news)

WO/2017/041720: Mevalonate pathway inhibitor as highly effective vaccine adjuvant
(Tsinghua University, published March 16, 2017)
Acetoacetyl-CoA transferase inhibitors, HMG-CoA synthase or reductase inhibitors, mevalonate or phosphomevalonate kinase inhibitors, mevalonate-5-pyrophosphate decarboxylase inhibitors, isopentenyl or farnesyl or geranylgeranyl pyrophosphate isomerase inhibitors, and geranylgeranyl transferase inhibitors are claimed.

WO/2017/035267: Method of treating Lennox-Gastaut syndrome using fenfluramine
(Zogenix International Ltd., published March 2, 2017)
From obesity to severe epilepsy: Lennox Syndrome patients are treated at a preferred dose of less than about 2.0 to about 0.01 mg/kg/day.

WO/2017/034315: Composition for preventing or treating mitochondrial diseases caused by immunosuppressants, and immune diseases, containing metformin
(The Catholic University of Korea Industry-Academic Cooperation Foundation, published March 2, 2017)
There seems to be no end to the alternate medical uses from the prototypical antidiabetic, metformin.

WO/2017/031319: Noradrenergic drug treatment of obstructive sleep apnea
(Massachusetts Institute of Technology, published February 23, 2017)
Relates to treatment using agents for promoting hypoglossal motoneuron excitability. Systemic yohimbine reversed the depressions of baseline hypoglossal activity and obstructive apnea-induced hLTF during REM sleep. BRL44408 (a selective antagonist for the α2A adrenoceptor) restored baseline hypoglossal activity, with pronounced facilitation during episodic airway occlusion.

WO/2017/027512: Use of laquinimod to treat traumatic brain injury
(Teva Pharmaceutical Industries, published February 16, 2017)
Laquinimod (which Teva dropped for multiple sclerosis in May 2017) promotes anti-inflammatory gene expression in microglia, downregulates inflammatory gene expression in microglia, and reduces apoptotic gene expression in microglia, reduces monocyte infiltration and axonal damage, increases microglial density, and improves balance and cognition in rats with TBI.

WO/2017/023047: Composition for preventing or treating inflammatory disease or cancer containing aripiprazole as an active ingredient
Sungkyunkwan University, publihed February 9, 2017)
In RAW264.7 cells treated with peptidoglycan, the antipsychotic aripiprazole concentration-dependently reduces nitric oxide and prostaglandin E2 production, and had an outstanding stomach damage suppressing effect in an in vivo inflammatory model. Also, it suppressed cancer cell proliferation in C6, U251, LN-428 and MDA-MB-231 cells.

WO/2017/020974: Dipeptidylpeptidase 4 inhibition enhances lymphocyte trafficking, improving both naturally occurring tumor immunity and immunotherapy
(Institut Pasteur, February 9, 2017)
In vivo post-translational processing of chemokines by DPP4 limits lymphocyte migration to sites of inflammation and tumors. Inhibition of DPP4 with sitagliptin (Merck & Co.’s Januvia®/Janumet®) enhanced tumor rejection by preserving biologically active CXCL10, and increasing trafficking into the tumor by lymphocytes expressing the counter-receptor CXCR3. Furthermore, DPP4 inhibition improved adjuvant-based immunotherapy, adoptive T cell transfer and checkpoint blockade.

WO/2017/017540: Therapeutic composition containing dipyridamole
(Remedeye, Inc. published February 2, 2017)
Topically administering to the eye an amount of the antithrombotic phosphodiesterase inhibitor, dipyridamole (Persantine®, Curantyl®) is effective in treatment of cataract and/or nevus and/or tumor lesion.

WO/2017/016880: Neurotoxin for use in the treatment of personality disorders
(Medizinische Hochschule Hannover, published February 2, 2017)
Botulinum toxin once again, this time for the treatment of an emotionally unstable personality disorder, impulse control and/or behavioral and emotional disorders with onset usually occurring in childhood and adolescence.

WO/2017/010382: Agent for treatment of myotonic dystrophy
(Osaka University, published January 19, 2017)
Erythromycin, clarithromycin, and azithromycin suppress the splicing abnormalities that are the cause of myotonic dystrophy and increase the normal splicing products.

WO/2017/009644: Kinase inhibitors for use in the treatment of fascioscapulohumeral dystrophy
(King’s College London, published January 19, 2017)
Sunitinib (Pfizer’s Sutent® cancer drug), vandetanib (Sanofi’s Caprelsa®, approved for advanced medullary thyroid cancer), and fedratinib (a JAK2 inhibitor that Sanofi used to develop for myeloproliferative diseases after acquiring its originator TargeGen) are claimed to be useful for this most disfiguring rare genetic disorder.

WO/2017/009136: Factor XIII for the treatment of interstitial cystitis
(Novo Nordisk Health Care AG, published January 19, 2017)
Fibrin-stabilizing factor preparations for this chronic bladder disease. That would be Novo Nordisk’s Tretten®/NovoThirteen®, or CSL Behring’s Corifact®.