On November 8, 2013 Patrys reported that it has been granted a second US patent for lead anti-cancer product PAT-LM1 (Press release Patrys, NOV 8, 2013, View Source [SID:1234500547]).
The United States Patent Office has issued the official "Letters Patent" on a key patent in the PAT-LM1 family; US patent 8,562,995 entitled "Neoplasm specific antibodies and uses thereof". It offers patent protection through to March 2024.
This is the second patent to be granted in the US jurisdiction, and the third for the PAT-LM1 family. In June this year a patent covering the use of the PAT-LM1 antibody or binding fragments for the treatment or prevention of metastasis was granted in New Zealand.
The patent claims the PAT-LM1 antibody and other variants comprising the Complementary Determining Region (CDRs) of the PAT-LM1 antibody.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

(Filing, 10-Q, Momenta Pharmaceuticals, NOV 8, 2013, View Source [SID:1234504029])

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

On November 5, 2013, the Company received written notification from the United States Food and Drug Administration (FDA) that its Phase 1 study of CUDC-427 has been placed on partial clinical hold following the report of death of a patient who progressed to liver failure approximately one month following the discontinuation of CUDC-427 dosing (Press release Curis, NOV 6, 2013, View Source [SID:1234500346]). Under this partial clinical hold, new patients may not be enrolled in the study until Curis provides the FDA with requested additional data and analysis on patients treated with CUDC-427 and a proposed protocol amendment is submitted to and accepted by the FDA. The Company expects to respond to the FDA’s requests for additional information and also plans to submit an amendment to the current protocol in a timely manner.
The current open-label, single-agent, dose escalation Phase 1 study of CUDC-427 was initiated in the third quarter of 2013 in patients with advanced and refractory solid tumors or lymphomas. The study was designed to determine the maximum tolerated dose (MTD) and recommended single-agent Phase 2 dose of CUDC-427 using a continuous, twice-daily treatment schedule. One patient with breast cancer metastatic to the liver, lungs, bone and ovaries developed serious adverse events related to liver function, including increases in serum levels of AST and ALT enzymes and bilirubin. Unlike prior clinical experience with CUDC-427, this patient’s liver enzyme levels did not recover in response to CUDC-427 discontinuation, and the patient died of liver failure approximately one month following the discontinuation of CUDC-427 dosing. While elevations in liver enzyme levels have previously occurred in patients receiving CUDC-427, no other patients in this or a prior Phase 1 CUDC-427 trial have experienced a serious adverse event of this nature. There are no patients currently being treated with CUDC-427 in this study as all other patients enrolled in this study have discontinued dosing due to disease progression or patient or physician discretion during the ordinary course of the study.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

On November 4, 2013 Cancer Research Technology (CRT), the commercial arm of Cancer Research UK, and Denmark-based drug discovery company Nuevolution A/S, reported to have signed a collaboration deal to discover anti-cancer drug molecules targeting several key proteins (Press release, Cancer Research Technology, APR 4, 2013, View Source [SID1234523248]).

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

The collaboration aims to identify drug leads that block the activity of a number of challenging cancer therapeutic targets. This could lead to the development of first-in-class novel treatments for cancer patients.

Through the partnership, drug candidate molecules which home in on selected targets will be identified by screening millions of diverse small molecules using Nuevolution’s proprietary Chemetics technology. This uses innovative DNA labelling to enable small molecule drug screening – a method to identify small molecules which bind to a target protein – on an unprecedented scale.

Thomas Franch, CSO of Nuevolution, said: "We are delighted to enter into this collaboration and believe that a strong synergy between the CRT and Nuevolution capabilities will provide for discovery traction on tough-to-drug targets.

CRT will provide expert information about the biology of the targets through Cancer Research UK’s network of world-class scientists. The first targets have already been approved by CRT and Nuevolution for entry into the collaboration.

In addition, CRT through its internal Discovery Laboratories will provide drug discovery expertise including in-vitro screening assays and cellular activity assays for the target proteins, to select the most promising molecules to develop as potential drugs.

The further pre-clinical development of any promising small molecules identified will form the basis of a separate deal to be agreed in the future between CRT and Nuevolution.

Dr Hamish Ryder, director of drug discovery at CRT’s Discovery Laboratories, said: "This deal is exciting as it will allow us to address a number of "low-tractability" cancer targets, which have proved difficult for ourselves and others to establish a foothold in drug discovery".

"This important partnership combines CRT’s drug discovery expertise and Cancer Research UK’s strong academic research base with powerful technology from Nuevolution to enable 100s of millions of compounds to be rapidly assessed – which we hope one day will be a starting point for new options for cancer patients and increased survival."

On November 1, 2013 Nimbus Discovery reported that it will present preclinical data at The Liver Meeting, the 64th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD), that show the company has optimized a unique series of Acetyl Co-A Carboxylase (ACC) allosteric inhibitors that bind to the BC domain of ACC and demonstrate excellent potency, drug-like properties and preclinical efficacy (Press release Nimbus Discovery, NOV 1, 2013, View Source [SID:1234501248]). The novel, internally-developed small molecules, ND-654 and ND-630, demonstrated desirable in vitro and in vivo efficacy in experimental models of metabolic disease, diabetes and hepatic steatosis. In an iterative design fashion over 16 months, the potency of this family of compounds were improved >1000x utilizing the company’s proprietary small molecule computational drug discovery technology, and drug-like properties were optimized to efficiently deliver development candidate quality molecules.

Schedule your 30 min Free 1stOncology Demo!
Discover why more than 1,500 members use 1stOncology™ to excel in:

Early/Late Stage Pipeline Development - Target Scouting - Clinical Biomarkers - Indication Selection & Expansion - BD&L Contacts - Conference Reports - Combinatorial Drug Settings - Companion Diagnostics - Drug Repositioning - First-in-class Analysis - Competitive Analysis - Deals & Licensing

                  Schedule Your 30 min Free Demo!

Simultaneous inhibition of both isoforms of ACC decreases fatty acid synthesis and stimulates fatty acid oxidation and has the potential to favorably affect the morbidity and mortality associated with obesity, diabetes, and fatty liver diseases including non-alcoholic steatohepatitis (NASH). Nimbus’ ACC inhibitors, including ND-654 and ND-630, are believed to be the first drug-like allosteric inhibitors to bind the biotin carboxylase (BC) domain of ACC with high potency and selectivity.

Key findings of the Nimbus compounds presented at the conference include:

ND-654
Liver specific ND-654 has favorable drug-like properties with a 2700:1 liver to muscle exposure
Proof-of-mechanism: ND-654 acutely inhibits ACC, with virtually no effect on muscle, resulting in focused pharmacological effects on the liver
Proof-of-concept: ND-654 demonstrated target engagement in the liver and dose dependently decreased fatty acid production in the liver
NC-630
Liver selective ND-630 has favorable drug-like properties with a 100:1 liver to muscle exposure
Proof-of-mechanism: ND-630 acutely inhibits ACC, demonstrating efficacy in both liver and muscle by preventing malonyl Co-A production
Proof-of-concept: ND-630 demonstrated target engagement in the liver and muscle
Dosing of ND-630 in high sucrose fed diet-induced obesity (DIO) rats showed improvement in insulin sensitivity, improvement in hepatic cholesterol and normalization of hepatic triglycerides, dose dependent decrease of plasma triglycerides and FFAs, and decrease in plasma cholesterol

"Within 16 months, Nimbus has become the first company to identify and optimize a broad portfolio of liver directed, small molecule inhibitors of ACC — a previously intractable disease target," said Rosana Kapeller, M.D., Ph.D., Chief Scientific Officer of Nimbus. "We are now preparing for ND-630 to enter the clinic in 2015 for the treatment of NASH and diabetes, while we continue to progress ND-654 in preclinical models of hepatocellular carcinoma."