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DRUG:

TW-37

i
Other names: TW-37
Associations
Trials
Company:
Ascenta
Drug class:
Bcl2 inhibitor, MCL1 inhibitor
Related drugs:
Associations
Trials
1year
Repurposing of investigational cancer drugs: Early phase discovery of dengue virus NS2B/NS3 protease inhibitors. (PubMed, Arch Pharm (Weinheim))
Mode of inhibition experiments and computational docking analyses indicated that ABT263 and ABT737 are competitive inhibitors, whereas AT101 and TW37 are noncompetitive inhibitors of the protease. With further evaluation, the identified inhibitors of the DENV NS2B/NS3 protease have the potential to be developed into specific anti-dengue therapeutics.
Journal
|
BCL2 (B-cell CLL/lymphoma 2)
|
navitoclax (ABT 263) • ABT-737 • TW-37
over1year
Retinal pigment epithelium exhibits gene expression and phagocytic activity alterations when exposed to retinoblastoma chemotherapeutics. (PubMed, Exp Eye Res)
Herein, we have developed two pluripotent stem cell (PSC)-RPE models to assess the cytotoxicity of known Rb chemotherapeutics such as Melphalan, Topotecan and TW-37. Together, our results demonstrate that although the most commonly used Rb chemotherapeutic drugs do not cause cytotoxicity in RPE, their application in vitro leads to compromised phagocytosis and strength of the barrier function, in addition to changes in gene expression that could alter the visual cycle in vivo. Our data demonstrate that widely used Rb chemotherapeutic drugs can have a deleterious impact on RPE cells and thus great care has to be exercised with regard to their delivery so the adjacent healthy RPE is not damaged during the course of tumor eradication.
Journal
|
topotecan • melphalan • TW-37
over1year
Codelivery of BCL2 and MCL1 Inhibitors Enabled by Phenylboronic Acid-Functionalized Polypeptide Nanovehicles for Synergetic and Potent Therapy of Acute Myeloid Leukemia. (PubMed, Adv Sci (Weinh))
Here, codelivery of BCL2 (ABT199) and MCL1 (TW37) inhibitors using phenylboronic acid-functionalized polypeptide nanovehicles to achieve synergetic and potent treatment of AML is adopted. In mice bearing MOLM-13-Luc or MV-411 AML cancer, NPAT reveal significant inhibition of tumor cell infiltration in bone marrow and main organs, potent suppression of tumor growth, and remarkably elevated mouse survival. With facile construction, varying drug combination, superior safety, synergetic efficacy, the phenylboronic acid-functionalized smart nanodrugs hold remarkable potential for AML treatment.
Journal
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BCL2 (B-cell CLL/lymphoma 2) • BCL2L11 (BCL2 Like 11)
|
MCL1 overexpression • MCL1 expression
|
Venclexta (venetoclax) • TW-37
over2years
pRB-Depleted Pluripotent Stem Cell Retinal Organoids Recapitulate Cell State Transitions of Retinoblastoma Development and Suggest an Important Role for pRB in Retinal Cell Differentiation. (PubMed, Stem Cells Transl Med)
In both models, the Rb cones expressed retinal ganglion and horizontal cell markers, a novel finding, which could help to better characterize these tumors with possible therapeutic implications. Application of Melphalan, Topotecan, and TW-37 led to a significant reduction in the fraction of Rb proliferating cone precursors, validating the suitability of these in vitro models for testing novel therapeutics for Rb.
Journal
|
RB1 (RB Transcriptional Corepressor 1)
|
topotecan • melphalan • TW-37
over2years
ROR2 increases the chemoresistance of melanoma by regulating p53 and Bcl2-family proteins via ERK hyperactivation. (PubMed, Cell Mol Biol Lett)
These results demonstrate that ROR2 contributes to melanoma progression by inhibiting apoptosis and increasing chemoresistance. These results not only position ROR2 as a marker of chemoresistance but also support its use as a novel therapeutic target in cancer.
Journal • IO biomarker
|
BCL2 (B-cell CLL/lymphoma 2) • MCL1 (Myeloid cell leukemia 1) • MDM2 (E3 ubiquitin protein ligase) • ROR2 (Receptor Tyrosine Kinase Like Orphan Receptor 2) • BAX (BCL2-associated X protein) • BID (BH3 Interacting Domain Death Agonist)
|
BAX expression
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Venclexta (venetoclax) • cisplatin • paclitaxel • dacarbazine • lomustine • ABT-737 • TW-37
over3years
Preclinical analysis of novel prognostic transcription factors and immune-related gene signatures for bladder cancer via TCGA-based bioinformatic analysis. (PubMed, Oncol Lett)
It was then verified that downregulation of FOSL1 can lead to an enhanced sensitivity of the TW37 in T24 bladder cancer cells. Overall, the present prognostic model demonstrated a robust capability of predicting OS of patients with BLCA. Hence, the gene markers identified could be applied for targeted therapies against BLCA.
Preclinical • Journal • Gene Signature
|
CD8 (cluster of differentiation 8) • CXCL13 (Chemokine (C-X-C motif) ligand 13) • EREG (Epiregulin) • EGR1 (Early Growth Response 1)
|
TW-37
almost4years
Synergistic Effects of TW-37 and ABT-263 on Renal Cell Carcinoma Cells. (PubMed, Cancer Manag Res)
Finally, TW-37 and ABT-263 also synergistically repressed the growth of RCC cells in xenograft mice. In summary, our data demonstrated that combined treatment with TW-37 and ABT-263 exhibited synergistic RCC cell death and this combination may be applied as an effective therapeutic strategy against RCC.
Journal
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BCL2 (B-cell CLL/lymphoma 2)
|
navitoclax (ABT 263) • TW-37
4years
Cryptotanshinone chemosensitivity potentiation by TW-37 in human oral cancer cell lines by targeting STAT3-Mcl-1 signaling. (PubMed, Cancer Cell Int)
Furthermore, TW-37 potentiated chemosusceptibility of cryptotanshinone in human oral cancer cell lines by suppressing STAT3-Mcl-1 signaling compared with either TW-37 or cryptotanshinone alone, resulting in potent apoptosis. This study not only unravels the single and chemosensitizing effects of TW-37 for treatment of human oral cancer but also highlights the likelihood of TW-37 as a good therapeutic strategy to enhance the prognosis of patients with oral cancer in the future.
Preclinical • Journal
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STAT3 (Signal Transducer And Activator Of Transcription 3)
|
MCL1 overexpression • MCL1 expression
|
TW-37
over4years
Antitumor effect of TW-37, a BH3 mimetic in human oral cancer. (PubMed, Lab Anim Res)
In vivo, TW-37 inhibited tumor growth in a nude mice xenograft model without any significant liver and kidney toxicities. Collectively, these data reveal that TW-37 may be a promising small molecule to inhibit human oral cancer.
Journal
|
BCL2 (B-cell CLL/lymphoma 2) • BCL2L1 (BCL2-like 1) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • CASP3 (Caspase 3)
|
TW-37