Xcytrin (motexafin gadolinum) / AbbVie - LARVOL DELTA

Profiling the Preclinical Pharmacokinetics and Biodistribution of a Platinum(IV)-Based Oxaliplatin Prodrug OxaliTEX and Their Significance to Antitumor Response. (PubMed, Mol Pharm) - "OxaliTEX (NOVO-111) is a novel gadolinium(III) texaphyrin-platinum(IV) complex that is under development for clinical trials. This suggests that other factors, such as the slow plasma terminal phase of the free Pt(II) species from oxaliTEX that prolongs exposure to low drug concentrations, may contribute to the favorable in vivo antitumor activity and therapeutic index of the conjugate. These characteristics demonstrate superiority of oxaliTEX and generate much optimism for its success in future clinical trials."

Journal • PK/PD data • Preclinical • Oncology • KRAS

Fibrin glue mediated direct delivery of radiation sensitizers results in enhanced efficacy of radiation treatment. (PubMed, Discov Oncol) - "Non-degraded RS was released from the FG for up to 72 h. FG-released 5FU greatly increased the efficacy of radiation therapy."

Journal • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor

Lutetium texaphyrin: A photocatalyst that triggers pyroptosis via biomolecular photoredox catalysis. (PubMed, Proc Natl Acad Sci U S A) - "The first control, gadolinium texaphyrin (MGd), is a weak photocatalyst but generates reactive oxygen species (ROS) efficiently...Even in the presence of a ROS scavenger, treating MDA-MB-231 cells with MLu at concentrations as low as 50 nM still allows for pyroptosis photo-activation. The present findings highlight how biomolecular photoredox catalysis could contribute to pyroptosis activation by mechanisms largely independent of ROS."

Journal • Oncology • CASP3 • GSDME

Inhibition of the thioredoxin system for radiosensitization therapy of cancer. (PubMed, Eur J Med Chem) - "Notable radiosensitizers, including gold nanoparticles (GNPs), gold triethylphosphine cyanide ([Au(SCN) (PEt3)]), auranofin, ceria nanoparticles (CONPs), curcumin and its derivatives, piperlongamide, indolequinone derivatives, micheliolide, motexafin gadolinium, and ethane selenide selenidazole derivatives (SeDs), are meticulously elucidated in terms of their applications in radiotherapy. In this review, the sensitization mechanisms and the current research progress of these radiosensitizers are discussed in detail, with the overall aim of providing valuable insights for the judicious application of Trx system inhibitors in the field of cancer radiosensitization therapy."

Journal • Review • Oncology

Myoglobin-loaded gadolinium nanotexaphyrins for oxygen synergy and imaging-guided radiosensitization therapy. (PubMed, Nat Commun) - "Gadolinium (Gd)-coordinated texaphyrin (Gd-Tex) is a promising radiosensitizer that entered clinical trials, but temporarily fails largely due to insufficient radiosensitization efficacy...In addition to Gd, the versatile Mb@Gd-NTs can also chelate Lu (Mb@Lu/Gd-NTs), enabling SPECT/MRI dual-modality imaging for accurately monitoring drug delivery in real-time. This "one-for-all" nanoplatform with the capability of chelating various trivalent metal ions exhibits broad clinical application prospects in imaging-guided radiosensitization therapy."

Journal • Oncology • MB

ACRIN6690: Contrast-Enhanced CT and MRI in Diagnosing and Staging Liver Cancer Using UNOS Policy (clinicaltrials.gov) - P=N/A | N=440 | Active, not recruiting | Sponsor: American College of Radiology Imaging Network | Trial completion date: Dec 2022 ➔ Dec 2023 | Trial primary completion date: Dec 2022 ➔ Dec 2023

Trial completion date • Trial primary completion date • Gastrointestinal Cancer • Hepatocellular Cancer • Hepatology • Liver Cancer • Oncology • Solid Tumor • Transplantation

Development of a Three-Dimensional Multi-Modal Perfusion-Thermal Electrode System for Complete Tumor Eradication. (PubMed, Cancers (Basel)) - "This new 3D, perfusion-thermal electrode system provided the evidence on the potential to enable simultaneous delivery of therapeutic agents and RF hyperthermia into the difficult-to-treat peritumoral zones, creating a new strategy to address the critical limitation, i.e., the high incidence of residual and recurrent tumor following thermal ablation of unresectable medium-to-large and irregular tumors."

Journal • Gastrointestinal Cancer • Hepatology • Liver Cancer • Oncology • Solid Tumor

Studying Repeated DCE-MRI and DWI in Patients Diagnosed With Prostate Cancer (clinicaltrials.gov) - P=N/A; N=30; Active, not recruiting; Sponsor: American College of Radiology Imaging Network; Trial completion date: Dec 2021 ➔ Dec 2022; Trial primary completion date: Dec 2020 ➔ Dec 2022

Clinical • Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • MRI

18F-DCFPyL PET/MRI in Regional Nodal&Distant Metastases Detection in Intermediate &HR Prostate Cancer (clinicaltrials.gov) - P; N=N/A; Available; Sponsor: Stanford University

Clinical • New trial • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

A new advanced in silico drug discovery method for novel coronavirus (SARS-CoV-2) with tensor decomposition-based unsupervised feature extraction. (PubMed, PLoS One) - "The drugs screened using our strategy may be effective candidates for treating patients with COVID-19."

Journal • Infectious Disease • Lung Cancer • Novel Coronavirus Disease • Oncology • Psychiatry • Solid Tumor

Studying Repeated DCE-MRI and DWI in Patients Diagnosed With Prostate Cancer (clinicaltrials.gov) - P=N/A; N=30; Active, not recruiting; Sponsor: American College of Radiology Imaging Network; Trial completion date: Dec 2019 ➔ Dec 2021; Trial primary completion date: Dec 2019 ➔ Dec 2020

Trial completion date • Trial primary completion date • Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor

Understanding of ROS-Inducing Strategy in Anticancer Therapy. (PubMed, Oxid Med Cell Longev) - "To understand the comprehensive biological response to certain prooxidative anticancer drugs such as 2-methoxyestradiol, buthionine sulfoximine, cisplatin, doxorubicin, imexon, and motexafin gadolinium, we propose and visualize the drug-gene, drug-cell process, and drug-disease interactions involved in oxidative stress induction and antioxidant process inhibition as well as specific side effects of these drugs using pathway analysis with a big data-based text-mining approach. Our review will be helpful to improve the therapeutic effects of anticancer drugs by providing information about biological changes that occur in response to prooxidants. For future directions, there is still a need for pharmacogenomic studies on prooxidative agents as well as the molecular mechanisms underlying the effects of the prooxidants and/or antioxidant-inhibitor agents for effective anticancer therapy through selective killing of cancer cells."

Journal • Review • Oncology

Oxaliplatin Pt(IV) prodrugs conjugated to gadolinium-texaphyrin as potential antitumor agents. (PubMed, Proc Natl Acad Sci U S A) - "A combination of tumor localization, redox cycling, and reversible protein binding is invoked to explain the relatively increased tolerability and enhanced anticancer activity seen in vivo. On the basis of the present studies, we conclude that metallotexaphyrin-Pt conjugates may have substantial clinical potential as antitumor agents."

Journal • Oncology • Solid Tumor

CPS1 expression and its prognostic significance in lung adenocarcinoma. (PubMed, Ann Transl Med) - "Through analysis of the dataset from the Gene Expression Omnibus (GEO) database, we found that the expression level of CPS1 was markedly downregulated in human A549 lung cancer cells treated with the chemotherapeutic drug motexafin gadolinium (MGd) in a time-dependent manner. Our work indicated that CPS1 is upregulated in LADC samples and that CPS1 might be used as a potential biomarker for the diagnostic and prognostic evaluation of LADC. Determining the detailed biological function of CPS1 in LADC tissues will provide promising and insightful information for our further study."

Journal • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • Thoracic Cancer

Motexafin Gadolinium in Treating Patients With Glioblastoma Multiforme Who Are Undergoing Radiation Therapy to the Brain (clinicaltrials.gov) - P1; N=N/A; Completed; Sponsor: National Cancer Institute (NCI); Suspended ➔ Completed

Clinical • Trial completion

Gadolinium Texaphyrin Plus Radiation Therapy in Treating Patients With Supratentorial Glioblastoma Multiforme (clinicaltrials.gov) - P1; N=6; Completed; Sponsor: Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins; N=18 ➔ 6

Clinical • Enrollment change

"#Biotech Best turnaround M&A $ARQL 20X $MRK BO in 2yr $ARRY $2s Multiple setbacks ➡️ 20X $PFE BO in 3yr $ECYT $1s Vintafolide fail ➡️ 20X $NVS BO in 1yr $MDVN $2s Dimebon fail ➡️ 40X $PFE BO in 6yr $PCYC 200X $ABBV BO in 6yr" (@AndyBiotech)

"#Biotech best turnaround M&A stories $ACHN $1s after HCV fail -> >$6/sh $ALXN BO $ECYT $1s after vintafolide fail -> $24/sh $NVS BO $MDVN $81/sh $PFE BO $PCYC $261/sh $ABBV BO Sometimes there's hope from ashes..." (@AndyBiotech)

Studying Repeated DCE-MRI and DWI in Patients Diagnosed With Prostate Cancer (clinicaltrials.gov) - P=N/A; N=30; Active, not recruiting; Sponsor: American College of Radiology Imaging Network; Trial completion date: Jan 2019 ➔ Dec 2019; Trial primary completion date: Jan 2019 ➔ Dec 2019

Clinical • Trial completion date • Trial primary completion date