- |||||||||| PLX038 / ProLynx, firtecan pegol (PEG-SN38) / Belrose, Rubraca (rucaparib) / Pharma& Schweiz
Enrollment closed, Enrollment change: PLX038 (PEGylated SN38) and Rucaparib in Solid Tumors and Small Cell Cancers (clinicaltrials.gov) - Dec 20, 2022
P1/2, N=10, Active, not recruiting,
Recruiting --> Active, not recruiting Recruiting --> Active, not recruiting | N=65 --> 10
- |||||||||| firtecan pegol (PEG-SN38) / Belrose
Journal: Pulmonary delivery of liposomes co-loaded with SN38 prodrug and curcumin for the treatment of lung cancer. (Pubmed Central) - Oct 15, 2022
SN38 was linked to cell-penetrating peptide (CPP) TAT via a polyethylene glycol (PEG) linker to form the SN38 prodrug (TAT-PEG-SN38)...The combination induced significant tumor inhibition in a BALB/c mouse lung cancer model. These results indicated that our SN38 prodrug and curcumin co-delivery system was a promising candidate for lung cancer treatment.
- |||||||||| firtecan pegol (PEG-SN38) / Belrose
Enrollment change, Trial termination: Study of EZN-2208 Pediatric Patients With Solid Tumors (clinicaltrials.gov) - Feb 14, 2022
P1/2, N=32, Terminated,
Active, not recruiting --> Terminated; Program suspended and divested N=24 --> 32 | Active, not recruiting --> Terminated; Program suspended and divested
- |||||||||| irinotecan / Generic mfg.
Journal: A Nanotherapeutic Strategy to Overcome Chemoresistance to Irinotecan/7-Ethyl-10-Hydroxy-Camptothecin in Colorectal Cancer. (Pubmed Central) - Jan 27, 2022
As the first nano-formulation of Ko143 and the first systemic co-delivery vehicle of SN38/CPT-11 and a BCRP inhibitor, BI@PEG-SN38 provides a new strategy for clinical development of SN38 and numerous "chemosensitizers", and exhibits promising applicability in precision cancer medicine. Panels of cancer cell lines established here provides a useful platform for BCRP- and cancer-related research and technology development.
- |||||||||| PLX038 / ProLynx, firtecan pegol (PEG-SN38) / Belrose, Rubraca (rucaparib) / Pharma& Schweiz
Enrollment change, Trial suspension: PLX038 (PEGylated SN38) and Rucaparib in Solid Tumors and Small Cell Cancers (clinicaltrials.gov) - Sep 29, 2021
P1/2, N=10, Suspended,
Panels of cancer cell lines established here provides a useful platform for BCRP- and cancer-related research and technology development. N=65 --> 10 | Recruiting --> Suspended
- |||||||||| firtecan pegol (PEG-SN38) / Zhejiang Hisun, Belrose
Journal: EZN-2208 treatment suppresses chronic lymphocytic leukaemia by interfering with environmental protection and increases response to fludarabine. (Pubmed Central) - Apr 27, 2021
Here, we tested the hypothesis that a pharmacological compound previously shown to inhibit HIF-1α may act as a chemosensitizer by interrupting protective microenvironmental interactions and exposing CLL cells to fludarabine-induced cytotoxicity. We found that the camptothecin-11 analogue EZN-2208 sensitizes CLL cells to fludarabine-induced apoptosis in cytoprotective in vitro cultures; in vivo EZN-2208 improves fludarabine responses, especially in early phases of leukaemia expansion, and exerts significant anti-leukaemia activity, thus suggesting that this or similar compounds may be considered as effective CLL therapeutic approaches.
- |||||||||| desferroxamine (DFO) / ZoneOne Pharma, PLX038 / ProLynx, firtecan pegol (PEG-SN38) / Zhejiang Hisun, Belrose
Journal: PET imaging of the EPR effect in tumor xenografts using small 15 nm diameter polyethylene glycols labeled with zirconium-89. (Pubmed Central) - Jan 13, 2021
PEG conjugates of the zirconium ligand desferroxamine B (DFB) of similar size and charge to PLX038 were prepared that contained one or four DFB, as well as one that contained three SN-38 moieties and one DFB...Compared to diagnostic liposomes, the PEG nanocarriers have a longer serum half-life, are retained in tumors at higher levels, remain there longer, and afford higher tumor exposure. The small PEG40kDa nanocarriers studied here show properties for passive targeting of tumors that are superior than most nanoparticles and might be effective probes to identify tumors susceptible to a similar size therapeutic nanocarriers such as PLX038.
- |||||||||| PLX038 / ProLynx, firtecan pegol (PEG-SN38) / Belrose, Rubraca (rucaparib) / Pharma& Schweiz
Trial completion date, Trial primary completion date: PLX038 (PEGylated SN38) and Rucaparib in Solid Tumors and Small Cell Cancers (clinicaltrials.gov) - Oct 26, 2020
P1/2, N=62, Recruiting,
The small PEG40kDa nanocarriers studied here show properties for passive targeting of tumors that are superior than most nanoparticles and might be effective probes to identify tumors susceptible to a similar size therapeutic nanocarriers such as PLX038. Trial completion date: Dec 2022 --> Dec 2024 | Trial primary completion date: Dec 2022 --> Dec 2023
- |||||||||| PLX038 / ProLynx, irinotecan / Generic mfg.
Journal: PLX038: a PEGylated prodrug of SN-38 independent of UGT1A1 activity. (Pubmed Central) - Jul 2, 2020
These results support the value of the single-mouse experimental design. The disposition of PEGylated SN-38 is independent of UGT1A activity in rats, and PLX038 may find utility in full-dose treatment of patients who are UGT1A1*28 homozygotes or have metastatic disease with coincidental or incidental liver dysfunction.
- |||||||||| firtecan pegol (PEG-SN38) / Zhejiang Hisun, Belrose, PT2385 / Merck (MSD)
[VIRTUAL] HIF2ALPHA PARTAKES TO AML DIFFERENTIATION BLOCKADE, AND ITS INHIBITION DRIVES AML DIFFERENTIATION () - May 16, 2020 - Abstract #EHA2020EHA_387;
Pro-differentiation activity of the specific HIF2α antagonist PT2385 was evaluated in AML cell lines, and ex vivo in AML cells from the bone marrow of 8 PDX models...Conclusion With this study, we defined a new role of HIF2α in the pathogenesis of AML, as a novel regulator of the AML differentiation blockade. Moreover, we suggest that HIF2α inhibition could be exploited as a new therapeutic avenue to treat AML, and to overcome resistance towards ATRA-induced differentiation therapy.
- |||||||||| PLX038 / ProLynx, firtecan pegol (PEG-SN38) / Belrose, Rubraca (rucaparib) / Pharma& Schweiz
Enrollment open: PLX038 (PEGylated SN38) and Rucaparib in Solid Tumors and Small Cell Cancers (clinicaltrials.gov) - Apr 8, 2020
P1/2, N=62, Recruiting,
Moreover, we suggest that HIF2α inhibition could be exploited as a new therapeutic avenue to treat AML, and to overcome resistance towards ATRA-induced differentiation therapy. Not yet recruiting --> Recruiting
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