- |||||||||| Amnolake (tamibarotene) / TMRC, Syros, Nippon Shinyaku, Zeria Pharma, Mylotarg (gemtuzumab ozogamicin) / UCB, PDL, Pfizer
Journal: Refractory acute promyelocytic leukemia with a complex karyotype (Pubmed Central) - Jan 14, 2022 Since the coordination of the unrelated donor had been completed at this time, she then underwent bone marrow transplantation with pre-conditioning of 4 Gy total body irradiation, fludarabine, and busulfan...APL usually has a good prognosis, and relapsed cases are often cured by autologous stem cell transplantation. However, this case was highly refractory to treatment and the patient deteriorated rapidly after the transplantation, suggesting a different pathogenesis from the usual from of APL.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, Zeria Pharma
Clinical, Journal: Defining the Transcriptional Control of Pediatric AML Highlights RARA as a Super-Enhancer Regulated Druggable Dependency. (Pubmed Central) - Jan 7, 2022 Tamibarotene prolonged 13 survival and suppressed the leukemia burden of a RARA SE-positive pAML patient-14 derived xenograft (PDX) mouse model compared to a RARA SE-negative PDX. Our work 15 demonstrates that examining chromatin regulation can identify new, druggable 16 dependencies in pAML and provides rationale for a pediatric tamibarotene trial in children 17 with RARA-high AML.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, Zeria Pharma
Journal: Tamibarotene inhibit the accumulation of fibrocyte and alleviate renal fibrosis by IL-17A. (Pubmed Central) - Oct 2, 2021 Furthermore, inhibition of IL-17A using Am80 (Tamibarotene) decreased fibrocytes and fibrocyte-associated chemokine and activator expression and significantly attenuated renal fibrosis in the UUO mice. Our findings suggest that Am80, which inhibits the accumulation of fibrocytes and alleviates renal fibrosis mediated by IL-17A, maybe a novel therapeutic drug for renal fibrosis.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, Zeria Pharma
Clinical, P1 data, Journal, Monotherapy: Phase I study of tamibarotene monotherapy in pediatric and young adult patients with recurrent/refractory solid tumors. (Pubmed Central) - Sep 22, 2021 Our findings suggest that Am80, which inhibits the accumulation of fibrocytes and alleviates renal fibrosis mediated by IL-17A, maybe a novel therapeutic drug for renal fibrosis. The recommended dose for phase II study of tamibarotene in pediatric and young adult patients with refractory solid tumors is 12 mg/m/day for 21 days in a 28 day cycle.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, Zeria Pharma
Journal: Computational repurposing of tamibarotene against triple mutant variant of SARS-CoV-2. (Pubmed Central) - Sep 19, 2021 Thus, in current research, molecular docking simulation-based virtual screening of a ligand library consisting of FDA-approved existing drugs followed by molecular dynamics simulation-based validation of leads was performed to develop a potent inhibitor molecule for the triple mutant viral strain SARS-CoV-2. Based on the safety profile, tamibarotene was selected as a safe and effective drug candidate for developing therapy against the triple mutant viral spike protein of SARS-CoV-2.
- |||||||||| Targretin oral (bexarotene oral) / ReXceptor
Journal: Acitretin and Retinoic Acid Derivatives Inhibit BK Polyomavirus Replication in Primary Human Proximal Renal Tubular Epithelial and Urothelial Cells. (Pubmed Central) - Aug 27, 2021 Retinoic acid-agonists (all-trans-retinoic acid, 9-cis-RA, 13-cis-RA, bexarotene, tamibarotene) and the RAR/RXR-antagonist RO41-5253 also inhibited BKPyV-replication, pointing to as yet undefined mechanism.ImportanceAcitretin selectively inhibits BKPyV-replication in primary human cell culture models of nephropathy and hemorrhagic cystitis. Since acitretin is an approved drug in clinical use reaching BKPyV-inhibiting concentrations in systemically treated patients, further studies are warranted to provide data for clinical repurposing of retinoids for treatment and prevention of replicative BKPyV-diseases.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, CytRx, Zeria
[VIRTUAL] SYSTEMIC MICROBIAL AGENTS INDUCE NEURODEGENERATION IN ALZHEIMER'S DISEASE MICE (On Demand Symposia A) - Dec 24, 2020 - Abstract #ADPD2021ADPD_537; Am580 markedly attenuated iNOS expression, inhibited reactive oxygen species and nitric oxide production, increased TREM2 expression and phagocytic activity, while maintaining microglial capacity for immune (cytokine) response. Conclusions Systemic colonization with microbial pathogens and systemic infections cause neurodegeneration in brains displaying amyloid pathology. Microglial modulation protects the hyper-susceptible AD brain from microbial TLRs -induced neurodegeneration.
- |||||||||| Venclexta (venetoclax) / Roche, AbbVie, Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, CytRx, Zeria
[VIRTUAL] Selection of RARA-Positive Newly Diagnosed Unfit AML Patients with Elevated RARA Gene Expression Enriches for Features Associated with Primary Resistance to Venetoclax and Clinical Response to SY‑1425, a Potent and Selective RARα Agonist, Plus Azacitidine (Poster Hall (Virtual Meeting)) - Nov 5, 2020 - Abstract #ASH2020ASH_3660; P2 In ND unfit AML, RARA+ pts, including those with clinical responses to SY-1425 plus Aza, are enriched for monocytic features associated with resistance to Ven. SY-1425 plus Aza shows potential as a novel targeted regimen for the treatment of RARA+ ND unfit AML and warrants further development in this genomically defined subset of AML pts who may be resistant to upfront SOC therapy with Ven.
- |||||||||| Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, CytRx, Zeria
Review, Journal: Strategies to generate functionally normal neutrophils to reduce infection and infection-related mortality in cancer chemotherapy. (Pubmed Central) - Jul 29, 2020 To date, CCIN-related infection and mortality remain a significant concern, as neutrophils generated in response to administered GCSF are functionally immature and cannot effectively fight infection. This review summarizes the molecular regulatory mechanisms of neutrophil granulocytic differentiation and innate immunity development, dissects the biology of GCSF in myeloid expansion, highlights the shortcomings of GCSF in CCIN treatment, updates the recent advance of a selective retinoid agonist that promotes neutrophil granulocytic differentiation, and evaluates the benefits of developing GCSF biosimilars to increase access to GCSF biologics versus seeking a new mode to fundamentally advance GCSF therapy for treatment of CCIN.
- |||||||||| ECT-001 / ExCellThera, Amnolake (retinobenzoic acid) / TMRC, Syros, Nippon Shinyaku, CytRx, Zeria
Journal: Effective and Rapid Generation of Functional Neutrophils from Induced Pluripotent Stem Cells Using ETV2-Modified mRNA. (Pubmed Central) - Jul 2, 2020 Neutrophils obtained in these conditions displayed a typical somatic neutrophil morphology, produced reactive oxygen species, formed neutrophil extracellular traps and possessed phagocytic and chemotactic activities. Overall, this technology offers an opportunity to generate a significant number of neutrophils as soon as 14 days after initiation of differentiation.
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