by hipockets | February 12, 2018 11:02 pm

This thread was initiated in order to provide a dedicated page for the members interested in following developing events at Aptose Biosciences. All posts made here should be about it. Other comments about biotech should be posted to the latest general purpose biotech thread, which on the date this is being written is https://www.stockgumshoe.com/2018/02/biotech-discussion-continued/[1] , or to the appropriate stock-specific threads.

As this is being written there are two discussion pages for $ARTH – https://www.stockgumshoe.com/2017/11/microblog-discussion-page-for-arch-therapeutics-arth/[2] and the original one, now closed to comments, started by AlanH http://www.stockgumshoe.com/2015/08/microblog-discussion-re-arth/[3] . There is also a special page for $AUPH started by LongOnLife: https://www.stockgumshoe.com/2018/02/microblog-discussion-page-for-aurinia-pharmaceuticals-auph/[4] .

Comments not suitable for any of the above threads can be posted to the latest clubhouse thread, which was started by AlanH and is now up to Volume 8.

Members posting to any of these threads are urged to follow the etiquette guidelines proposed by AlanH several years ago.

With that bit of housekeeping out of the way, I’m interested in APTO because it’s working on drugs to treat acute myeloid leukemia (AML). My “favorite daughter”, my only child, died from it six years ago just before Christmas and 104 weeks after her daughter, another only child, was born.. At that time, only about 7 % of people diagnosed with it lived longer than 2 years. Diana did not make it that far, although she fought it ferociously by undergoing 2 rounds of chemo and two bone marrow transplants.

Studying AML is just one of Aptose’s programs; the others can be found in the information below.

APTO was introduced to the biotech threads by Dr. KSS on 12/16/16 in the thread THE TWELVE BIOTECHS OF CHRISTMAS: ONE , http://www.stockgumshoe.com/2016/12/the-twelve-biotechs-of-christmas-one/[5] . His comments, from then till 7/13/17, are documented on the Misc Op tab of the spreadsheet at http://tinyurl.com/KSSDAMAN[6] . I will try to include the later comments soon.

From the company’s website http://aptose.com/[7] :

Aptose Biosciences employs a mechanism-driven approach to deliver
safer, targeted, first-in-class cancer drugs and diagnostics.

“Aptose Biosciences is a science-driven biotechnology company advancing first-in-class agents to treat life-threatening cancers, such as acute myeloid leukemia (AML), high-risk myelodysplastic syndromes (MDS) and other hematologic malignancies. Based on insights into the genetic and epigenetic profiles of certain cancers and patient populations, Aptose is building a pipeline of novel oncology therapies directed at dysregulated processes and signaling pathways. Aptose is developing targeted medicines for precision treatment of these diseases, based on a patient’s specific gene expression signature. In the treatment of cancer, this strategy is intended to optimize efficacy and quality of life by minimizing the cytotoxic side effects associated with conventional therapies.

“CG026806 (CG’806) is a highly potent first-in-class pan-FLT3/BTK inhibitor. This small molecule therapeutic agent, exhibits a picomolar IC50 toward the FMS-like tyrosine kinase 3 with the Internal Tandem Duplication (FLT3-ITD) and significant potency against other mutant forms of FLT3. Because of the potency of CG’806 against the FLT3 enzyme, it may become an effective therapy for AML patients, including the subset of patients having the FLT3-ITD, which occurs in approximately 30% of patients with AML and is associated with poor prognosis. Importantly, CG’806 targets other oncogenic kinases which may also be operative in AML, thereby potentially allowing the agent to become an important therapeutic option for a difficult-to-treat patient population.

“In addition to potent inhibition of wild type and mutant forms of the FLT3 enzyme, CG’806 is a highly potent, reversible, non-covalent inhibitor of the wild type and mutant forms of the BTK enzymes. Overexpression of BTK drives certain B cell malignancies, including chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), diffuse large B cell lymphoma (DLBCL) and others. Treatment of such B cell malignancies with covalent BTK inhibitors that target the cysteine residue in the active site of BTK can lead to drug resistance via mutation of the cysteine amino acid residue to a serine residue (BTK-C481S mutant). CG’806 targets the ATP-binding pocket of BTK through a reversible, non-covalent mechanism, thereby allowing CG’806 to retain low nM potency against the BTK-C481S mutant enzyme. Thus, CG’806 may serve as a novel therapeutic agent to treat B cell malignancy patients that are refractory, resistant or intolerant to covalent BTK inhibitors.

“APTO-253, the Company’s second program, is a small molecule therapeutic agent that inhibits expression of the c-Myc oncogene without causing general myelosuppression of the bone marrow. The c-Myc oncogene is overexpressed in hematologic cancers, including AML. C-Myc is a transcription factor that regulates cell growth, proliferation, differentiation and apoptosis, and overexpression amplifies new sets of genes to promote oncogenesis. APTO-253 dramatically downregulates expression of the c-Myc oncogene in AML cells and depletes those cells of the c-Myc oncoprotein, leading to apoptotic cell death in AML cells. Thus APTO-253 may serve as safe and effective c-Myc inhibitor for AML that combines well with other agents and does not impact the normal bone marrow.
Aptose’s leadership team comprises accomplished industry, financial and clinical research professionals who are dedicated to building a comprehensive anticancer drug pipeline and clinical development programs focused on targeted therapeutics directed against dysregulated oncogenic processes in patients with life-threatening hematologic malignancies.”

I have no position in $APTO at the moment. All of my stocks were deeply in the red last week, but I will take a full position as soon as I can figure out what to sell. In the meantime, I look forward to everybody’s input on their thinking about $APTO.

  1. https://www.stockgumshoe.com/2018/02/biotech-discussion-continued/: https://www.stockgumshoe.com/2018/02/biotech-discussion-continued/
  2. https://www.stockgumshoe.com/2017/11/microblog-discussion-page-for-arch-therapeutics-arth/: https://www.stockgumshoe.com/2017/11/microblog-discussion-page-for-arch-therapeutics-arth/
  3. http://www.stockgumshoe.com/2015/08/microblog-discussion-re-arth/: http://www.stockgumshoe.com/2015/08/microblog-discussion-re-arth/
  4. https://www.stockgumshoe.com/2018/02/microblog-discussion-page-for-aurinia-pharmaceuticals-auph/: https://www.stockgumshoe.com/2018/02/microblog-discussion-page-for-aurinia-pharmaceuticals-auph/
  5. http://www.stockgumshoe.com/2016/12/the-twelve-biotechs-of-christmas-one/: http://www.stockgumshoe.com/2016/12/the-twelve-biotechs-of-christmas-one/
  6. http://tinyurl.com/KSSDAMAN: http://tinyurl.com/KSSDAMAN
  7. http://aptose.com/: http://aptose.com/

Source URL: https://www.stockgumshoe.com/2018/02/microblog-discussion-page-for-apto/

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