mipicoledine (DM-CHOC-PEN) / DEKK-TEC - LARVOL DELTA

Preclinical Activity of 4-Demethyl-4-cholesteryloxycarbonylpenclomedine in Melanoma. (PubMed, Anticancer Res) - "Longer survival was seen with DM-CHOC-PEN in a C57BL murine model relative to temozolomide and saline-treated controls, supporting the development of clinical trials assessing the efficacy of DM-CHOC-PEN as treatment for metastatic melanoma."

Journal • Preclinical • Brain Cancer • Breast Cancer • CNS Tumor • Glioma • Immune Modulation • Melanoma • Oncology • Solid Tumor

[VIRTUAL] Early Phase II clinical trial results for 4-demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) in adolescents and young adults (AYA) with brain cancers (AACR-NCI-EORTC 2021) - No abstract available

Clinical • P2 data • Brain Cancer • Oncology • Solid Tumor

DM-CHOC-PEN Plus Radiation for Brain Tumors (clinicaltrials.gov) - P1 | N=19 | Completed | Sponsor: DEKK-TEC, Inc. | Recruiting ➔ Completed | Trial completion date: Dec 2021 ➔ Oct 2022 | Trial primary completion date: Dec 2021 ➔ Oct 2022

Trial completion • Trial completion date • Trial primary completion date • Brain Cancer • Oncology • Solid Tumor

Use of 4-demethyl-4-cholesteryloxycarbonyl-penclomedine (DM-CHOC-PEN) as therapy for advanced non-small cell lung cancer (NSCLC) involving the CNS (AACR 2022) - "DM-CHOC-PEN is a bis-alkylator of DNA that is safe at the dose levels described and has produced long term objective responses with manageable toxicities and improved quality of life in subjects with NSCLC involving the CNS lacking genetic rearrangements or tumor targets and/or had failed standard therapies. Complete data on subject responses and observed toxicities will be presented. Supported by NCI/SBIR grants - R43/44CA132257 and NIH NIGMS 1 U54 GM104940 - the latter supports the Louisiana Clinical and Translational Science Center, New Orleans, LA"

Brain Cancer • CNS Tumor • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

DM-CHOC-PEN for Brain Tumors in AYA Subjects (clinicaltrials.gov) - P2; N=20; Completed; Sponsor: DEKK-TEC, Inc.; Recruiting ➔ Completed; Trial completion date: Dec 2021 ➔ Sep 2021; Trial primary completion date: Dec 2021 ➔ Aug 2021

Clinical • Trial completion • Trial completion date • Trial primary completion date • Brain Cancer • Oncology • Solid Tumor • MRI

"DNAのグアニンとシトシンをアルキル化することでDNAを損傷させ効果を発揮するDM-CHOC-PENが、青少年（AYA）世代の中枢神経系の腫瘍（脳転移を含む）に有効である可能性が報告されました。 #脳腫瘍 #脳転移 #AYA #Targets21 https://t.co/YSzv3a5slm" (@cancer_navi)

Oncology

Early phase I clinical trial results for 4-demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) plus radiation in cancers involving the CNS (AACR 2018) - "Preliminary data is presented that supports enhanced cytotoxicity and safety of DM-CHOC-PEN plus radiation as therapy for subjects with cancers involving the CNS. Observations during Phase I/II clinical trials with DM-CHOC-PEN alone support the drugs persistent presence in human tumors after systemic administration and possible positive effects on response to subsequent radiation. Complete data on subject responses and observed toxicities will be presented."

Clinical • P1 data • Melanoma • Non Small Cell Lung Cancer • Sarcoma

[VIRTUAL] Phase I Clinical Trial: Results from the Use of 4-demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) plus Radiation as Treatment for Cancers involving the CNS (ASTRO 2020) - "Data is presented that documents effectiveness and safety of DM-CHOC-PEN plus radiation as therapy for subjects with cancers involving the CNS. Observations during this trial supported the drug’s ability to penetrate human tumors involving the CNS and acceptabity as a method to improving responses to radiation. Complete data on subject responses and observed toxicities will be presented."

Clinical • P1 data • Astrocytoma • CNS Tumor • Genito-urinary Cancer • Lung Cancer • Melanoma • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Sarcoma • Solid Tumor

[VIRTUAL] Phase I/II clinical trial results for 4-demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) as treatment for adolescents and young adults (AYA) with cancers involving the CNS (AACR-I 2020) - "DM-CHOC-PEN is safe in doses of 39 – 98.7 mg/m2 and has produced objective responses with manageable toxicities in AYA subjects with cancer involving the CNS. Complete data on subject responses and observed toxicities will be presented. We propose a 3-stage mechanism for drug entry into the CNS and into cancer cells via reversible binding with RBCs and then association with L-glutamine transport into cells."

Clinical • P1/2 data

[VIRTUAL] Phase I clinical trial: results from the use of 4-demethyl-4 cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) plus radiation as treatment for cancers involving the CNS (AACR-I 2020) - "Data is presented that documents effectiveness and safety of DM-CHOC-PEN plus radiation as therapy for subjects with cancers involving the CNS. Observations during this trial supported the drug’s ability to penetrate human tumors involving the CNS and acceptability as a method to improving responses to radiation. Complete data on subject responses and observed toxicities will be presented."

Clinical • P1 data

[VIRTUAL] Phase II clinical trial results for 4-demethyl-4-cholesteryloxycarbonyl-penclomedine (DM-CHOC-PEN) in advanced non-small cell lung cancer (NSCLC) involving the CNS (AACR 2021) - "DM-CHOC-PEN is a bis-alkylator of DNA that is safe at the dose levels described and has produced long term objective responses with manageable toxicities in subjects with NSCLC involving the CNS lacking genetic rearrangements or tumor targets and/or had failed standard therapies. Complete data on subject responses and observed toxicities will be presented. A 3-stage mechanism is proposed for drug entry into the CNS and into NSCLC cells via reversible binding with RBC’s and then associated with L-glutamine transport into cells."

Clinical • P2 data • Brain Cancer • CNS Tumor • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

A Phase I clinical trial: Use of 4-demethyl-4-cholesteryl- oxycarbonyl-penclomedine (DM-CHOC-PEN) plus radiation as treatments for cancers involving the CNS (AACR 2019) - "Data is presented that documents effectiveness and safety of DM-CHOC-PEN plus radiation as therapy for subjects with cancers involving the CNS. Observations during Phase I/II clinical trials with DM-CHOC-PEN alone supported the drug’s persistent presence in human tumors after systemic administration and possible positive effects on response to subsequent radiation. Complete data on subject responses and observed toxicities will be presented."

Clinical • P1 data

Study of 4-Demethyl-4-cholesteryloxycarbonylpenclome (DM-CHOC-PEN) in Patients With Brain Tumors (clinicaltrials.gov) - P2; N=29; Completed; Sponsor: DEKK-TEC, Inc.; Trial completion date: Jun 2016 ➔ Aug 2020

Clinical • Trial completion date • Brain Cancer • Breast Cancer • Glioblastoma • Lung Cancer • Oncology • Solid Tumor

DM-CHOC-PEN Plus Radiation for Brain Tumors (clinicaltrials.gov) - P1; N=18; Recruiting; Sponsor: DEKK-TEC, Inc.; Trial completion date: Dec 2018 ➔ Dec 2021; Trial primary completion date: Dec 2018 ➔ Dec 2021

Clinical • Trial completion date • Trial primary completion date • Brain Cancer • Oncology • Solid Tumor

DM-CHOC-PEN for Brain Tumors in AYA Subjects (clinicaltrials.gov) - P2; N=20; Recruiting; Sponsor: DEKK-TEC, Inc.; Not yet recruiting ➔ Recruiting

Clinical • Enrollment open • Brain Cancer • Oncology • Solid Tumor • MRI

Support for 4-demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) as a magnetic field effort sensitizer in NSCLC (AACR-NCI-EORTC 2019) - "DM-CHOC-PEN is polarized in a magnetic field with shifting of electron flux toward the polychlorinated pyridine ring and weakening the carbonate link facilitating its reactivity with H2O (hydrolysis) and the loss of the cholesteryl carbonate moiety, resulting in the release of the active specie – DM-PEN. DM-PEN is involved in DM-CHOC-PEN’s second phase of DNA alkylation. Thus, the ‘controlled release’ of the active specie in magnetic fields potentiates cytotoxicity and ultimately may reduce the amount of drug required for effective anti-cancer activity."