kt-3000 series / Rakovina Therap - LARVOL DELTA

Small-molecule bifunctional inhibitors of PARP1/2 and HDAC enzymes (EORTC-NCI-AACR 2024) - "PARPi combined with HDACi has shown enhanced efficacy in pre-clinical studies in various cancers, and a clinical trial of olaparib and vorinostat against metastatic breast cancer is ongoing. kt-3000 molecules demonstrate potent inhibition of PARP1/2 and HDAC activities. Further development of these bifunctional single-molecule inhibitors may offer a novel therapeutic opportunity for treatment of cancers with and without DNA damage repair defects."

Breast Cancer • Ewing Sarcoma • Oncology • Sarcoma • Solid Tumor • BRCA

Rakovina Therapeutics Announces Private Placement Offering (GlobeNewswire) - "Rakovina Therapeutics Inc...is pleased to announce a non-brokered private placement offering (the 'Offering') of up to $1.25 million...The Company plans to use the proceeds to continue the discovery and advancement of novel cancer treatments by leveraging collaborations with two proprietary Artificial Intelligence (AI) platforms: the Deep Docking AI platform and the Variational AI Enki Platform. The Company also plans to continue the development of its kt-3000 series through collaborations and partnerships with biotech and pharma companies."

Financing • Oncology

Rakovina Therapeutics to Present Research Highlighting Small-Molecule Bifunctional Inhibitors of PARP1/2 and HDAC Enzymes at the 36th EORTC-NCI-AACR Symposium in Barcelona Spain (GlobeNewswire) - "Rakovina’s novel class of bifunctional small molecule compounds, known as kt-3000 series, has demonstrated potent dual inhibition of PARP1/2 and HDAC enzymes in preclinical studies. Compared to single-function inhibitors such as olaparib (PARP) and vorinostat (HDAC), dual-function kt-3000 compounds demonstrate greater potency against both HR-deficient and proficient cancer cells."

Preclinical • Oncology

Pharmacological synthetic lethality by co-inhibition of PARP and HDAC enzymes (AACR 2024) - "Dual PARP-HDAC inhibition decreased survival of HR-proficient cells in both 2D cultures and 3D spheroid assays with lower EC50 values than olaparib or vorinostat alone. Combination of PARP inhibition and HDAC inhibition showed increased efficacy compared to single agent PARP inhibition in HR-proficient cells. Development of bifunctional inhibitors may provide a novel therapeutic opportunity for tumors with limited response rates to single agent PARPi."

Late-breaking abstract • Synthetic lethality • Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • BRCA • BRCA1 • BRCA2 • PARP2

Rakovina Therapeutics Inc. Announces Q3 2023 Financial Results and Provides Corporate Update (GlobeNewswire) - "During the past quarter, we have continued preclinical research activities with the aim of advancing a lead candidate from our kt-3000 series program into human clinical trials during 2024. In October 2023, we presented additional data from our kt-3000 series at the AACR-NCI-EORTIC Molecular Targets and Therapeutics Meeting. These data demonstrate the potential of kt-3000 series drug candidates to treat cancers that are resistant to first-generation PARPi and potential to address unmet medical needs in the treatment of a range of cancers including leukemia, breast cancer, liver cancer, glioblastoma, prostate cancer, Ewing sarcoma and anaplastic thyroid cancer."

New trial • Preclinical • Breast Cancer • Ewing Sarcoma • Glioblastoma • Leukemia • Liver Cancer • Prostate Cancer • Thyroid Gland Carcinoma

A bi-functional PARP-HDAC inhibitor with activity in Ewing sarcoma. (PubMed, Clin Cancer Res) - "Our data demonstrates the preclinical justification for studying the benefit of dual PARP and HDAC inhibition in the treatment of Ewing sarcoma in a clinical trial and provides proof-of-concept for a bi-functional single-molecule therapeutic strategy."

Journal • Ewing Sarcoma • Oncology • Sarcoma • Solid Tumor

Rakovina Therapeutics Inc. Announces Closing of $1.5 Million Convertible Debenture Financing (GlobeNewswire) - "Rakovina Therapeutics...is pleased to announce that it has closed its previously announced non-brokered private placement (the 'Offering') of unsecured convertible debenture units of the Company (the 'Debenture Units') for aggregate gross proceeds to the Company of approximately $1.5 million....Rakovina intends to use the net proceeds of the Offering for research and development expenses primarily to advance its lead kt-3000 dual function DNA-damage response inhibitor program toward human clinical trials and for general working capital purposes."

Financing • Oncology • Solid Tumor

Rakovina Therapeutics Announces Presentation of New kt-3000 Series Data at AACR Annual Meeting (GlobeNewswire) - "Data presented at the meeting demonstrate that Rakovina Therapeutics' kt-3000 prototype lead candidate exhibits higher PARP-1 vs. PARP-2 selectivity compared to the FDA-approved PARP inhibitor, olaparib. Selectivity against PARP1 is believed to correlate with an improved safety profile vs. first-generation PARP inhibitors....The data also demonstrate that the dual functional kt-3000 prototype lead candidate is more effective against Ewing sarcoma tumor cells than either a PARP inhibitor or HDAC inhibitor alone....The kt-3000 lead candidate effectively reduced lung metastases in mice inoculated with Ewing sarcoma tumor cells."

Preclinical • Ewing Sarcoma • Oncology • Sarcoma • Solid Tumor

Rakovina Therapeutics Announces Presentation at the 6th Annual DDR-inhibitors Summit (GlobeNewswire) - “Rakovina Therapeutics Inc…is pleased to announce a scientific presentation at the 6^th Annual DDR Inhibitors Summit in Boston, MA….Professor Mads Daugaard, president & chief scientific officer of Rakovina Therapeutics Inc. presented an address…in which he described the company’s research results with its novel kt-3000 series in pre-clinical models of Ewing sarcoma, a rare childhood tumor. The data demonstrated that co-inhibition of PARP and HDAC amplifies DNA damage and cytotoxicity in cancer cells. An FDA approved PARP inhibitor has previously been tested in a phase II clinical study in Ewing sarcoma where it failed to produce durable responses. Prof. Daugaard reported that Ewing sarcoma cancer cells are highly sensitive to treatment with combination PARP-HDAC inhibition exhibited by kt-3000 drug candidates.”

Preclinical • Ewing Sarcoma • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

Rakovina Therapeutics Inc. Announces Q3 2022 Financial Results and Provides Corporate Update (GlobeNewswire) - "On November 14, 2022, the Company announced the preprint publication of a manuscript entitled ‘A bi-functional PARP-HDAC inhibitor with activity in Ewing sarcoma’. The manuscript reports research results of our kt-3000 dual PARP-HDAC inhibitor drug candidate in HR-proficient Ewing sarcoma models....In an Ewing sarcoma metastasis model, a kt-3000 drug candidate prevented metastatic cancer growth in the lungs of mice inoculated with an aggressive Ewing sarcoma cell line....'Based on our progress to date, we are confident that we may be in a position to file regulatory documentation to begin human clinical trials with a kt-3000 series drug candidate in the second half of 2023'."

New trial • Preclinical • Ewing Sarcoma • Oncology • Sarcoma • Solid Tumor

Rakovina Therapeutics Announces Preclinical Data Presentation at the 34th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium (GlobeNewswire) - "Rakovina Therapeutics...is pleased to announce the presentation of new data during the 34th EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium, which was held in Barcelona Spain October 26-28, 2022....'Data presented at the conference demonstrate our continued progress toward confirmation of a lead compound from our kt-3000 series for advancement to human clinical trials'..."

Preclinical • Oncology

Rakovina Therapeutics Presents Preclinical Data on its Novel kt-3000 Series at the 2022 AACR Special Conference on Sarcomas (GlobeNewswire) - "New kt-3000 data presented by Rakovina Therapeutics’ researchers at the AACR Special Conference on Sarcomas demonstrate that:...Rakovina Therapeutics’ kt-3283 prototype lead drug candidate exhibits potent bi-functional activity as evidenced by inhibition of PARP and PARylation at a low nanomolar potency plus potent inhibition of HDAC enzyme activity; kt-3283 treatment reduced viability of Ewing sarcoma cells >25 fold more potently than an FDA-approved PARP inhibitor or FDA-approved HDAC inhibitor"

Preclinical • Ewing Sarcoma • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

Rakovina Therapeutics to Present Abstract at the 2022 AACR Special Conference – Sarcomas (GlobeNewswire) - "Rakovina Therapeutics Inc....is pleased to announce the acceptance of an abstract to be presented at the 2022 AACR Special Conference on Sarcomas. The conference is being held May 9-12, 2022 in Montreal, Canada. Rakovina Therapeutics’ presentation entitled In vitro efficacy of a novel dual PARP-HDAC Inhibitor in Ewing sarcoma will highlight the Company’s development of its novel kt-3000 series drug candidates as a potential treatment of sarcomas and soft tissue tumors."

Preclinical • Ewing Sarcoma • Oncology • Sarcoma • Soft Tissue Sarcoma • Solid Tumor

Rakovina Therapeutics Partners with St. Baldrick’s Foundation to Research and Develop New Treatments for Childhood Bone Cancer (GlobeNewswire) - "Rakovina Therapeutics...announced that the Company has been selected to join a three year US$975,000 (CDN1,297,000) research program funded by the St. Baldrick’s Foundation Martha’s BEST Grant for All, which is aimed at developing new treatments for Ewing sarcoma, an aggressive bone and soft tissue cancer in children and young adults....Funding from the St. Baldrick’s Foundation will support pre-clinical IND-enabling research conducted at the University of British Columbia over the next 12 months."

Financing • Oncology

Rakovina Therapeutics Presents at the 6th biennial Canadian Cancer Research Conference (GlobeNewswire) - "Rakovina Therapeutics presented a poster presentation entitled In Vitro Activity of Novel Dual PARP-HDAC Inhibitors, which described results of the Company’s research related to the development of its novel kt-3000 series novel drug candidates....In summary, the data suggests promising activity for kt-3000 series compounds against both BRCA wild-type and BRCA mutant cancers, benchmarked against an FDA-approved PARP inhibitor."

Preclinical • Oncology

Rakovina Therapeutics to Present at the 6th biennial Canadian Cancer Research Conference (GlobeNewswire) - "Rakovina Therapeutics Inc...announced that the Company has been invited to present a poster presentation at the sixth biennial Canadian Cancer Research Conference (CCRC), which is being held virtually November 8-11, 2021....During the meeting, Rakovina Therapeutics researchers will present an update on lead optimization activities with the Company’s novel kt-3000 series."

Clinical • Oncology

Rakovina Therapeutics Presents at the 2021 AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics (GlobeNewswire) - "Rakovina Therapeutics Inc...today announced a summary of the Company’s presentation at the 2021 AACR-NCI-EORTC Virtual International Conference on Molecular Targets and Cancer Therapeutics, which was held virtually on October 7-10, 2021...The kt-3000 series are novel drug candidates that combine inhibition of poly (ADP-ribose) polymerase (PARP) and histone deacetylase (HDAC) into a single molecule...Laboratory studies demonstrate that HDAC inhibition degrades BRCA1 in cells that have become resistant to PARP inhibitors, which has been shown to re-sensitize resistant cancers to PARP-inhibitor treatment."

Preclinical • Oncology

[VIRTUAL] In Vitro Activity and Efficacy of Novel Dual PARP-HDAC Inhibitors (AACR-NCI-EORTC 2021) - No abstract available

Preclinical • Oncology

Rakovina Therapeutics Presents Preclinical Data on novel kt-3000 Series Drug Candidates at JCA-AACR Precision Medicine International Conference (GlobeNewswire) - "Rakovina Therapeutics presented data in a video presentation entitled In Vitro Activity of Novel Dual PARP-HDAC Inhibitors. The Company’s novel kt-3000 series is a dual inhibitor of poly (ADP-ribose) polymerase (PARP) and histone deacetylase (HDAC). Publications to date have shown potential synergy between PARP inhibitors and HDAC inhibitors and the combination has been shown to sensitize PARP-inhibitor resistant cells to treatment in vitro."

Preclinical • Oncology

Rakovina Therapeutics to Present at the JCA-AACR Precision Medicine International Conference (GlobeNewswire) - "Rakovina Therapeutics...is pleased to announce that its abstract entitled In Vitro Activity of Novel Dual PARP-HDAC Inhibitors has been accepted for presentation at the inaugural JCA-AACR Precision Medicine Conference being held virtually on September 10-12, 2021 (US) and September 11-13 (Japan)."

Preclinical • Oncology