The rolling submission to FDA for darolutamide in the U.S. completed

On February 27, 2019 Orion Corporation and Bayer reported the completion of the rolling submission of a New Drug Application (NDA) for darolutamide to the U.S. Food and Drug Administration (FDA) (Press release, Bayer, FEB 27, 2019, View Source [SID1234533747]).

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The submission, which was initiated in December 2018, is based on data from the Phase III ARAMIS trial in men with non-metastatic castration-resistant prostate cancer (nmCRPC) showing a statistically significant improvement in metastasis-free survival (MFS) for darolutamide plus androgen deprivation therapy (ADT). Darolutamide plus ADT has shown a favorable safety profile compared to placebo plus ADT.1 These data were recently presented at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Genitourinary Cancers Symposium (ASCO GU) in San Francisco and published simultaneously in The New England Journal of Medicine.

"Darolutamide is highly effective in the patient population with non-metastatic castration-resistant prostate cancer, and it has a side-effect profile that parallels that of placebo. Patients who received Darolutamide had substantially longer MFS in the ARAMIS trial, and there was also a strong trend for improved overall survival. These results are truly exciting. We are looking forward to taking the next steps in bringing Darolutamide to men with nmCRPC and their treating physicians", said Christer Nordstedt, MD, PhD, Senior Vice President, Research and Development, Orion Corporation.

Bayer has been granted Fast Track designation by the U.S. Food and Drug Administration (FDA) for darolutamide in men with nmCRPC. Bayer is also in discussions with other health authorities regarding a submission of darolutamide. The compound is being developed jointly by Orion Corporation and Bayer.

About ARAMIS

The ARAMIS trial is a randomized, Phase III, multi-center, double-blind, placebo-controlled trial evaluating the safety and efficacy of oral darolutamide in patients with nmCRPC who are currently being treated with ADT and are at high risk for developing metastatic disease. 1,509 patients were randomized in a 2:1 ratio to receive 600 mg of darolutamide twice a day or placebo along with ADT.

About darolutamide

Darolutamide is a non-steroidal androgen receptor antagonist with a distinct chemical structure that binds to the receptor with high affinity and exhibits strong antagonistic activity, thereby inhibiting the receptor function and the growth of prostate cancer cells. In preclinical studies, darolutamide demonstrated lower blood-brain barrier penetration compared to other currently available AR antagonists. This may also explain the overall low incidence of central nervous system (CNS)-related adverse events seen in the ARAMIS Phase III study.

In addition to the Phase III trial ARAMIS in men with nmCRPC, darolutamide is also being investigated in a Phase III study in metastatic hormone-sensitive prostate cancer (ARASENS). Information about these trials can be found at www.clinicaltrials.gov.

Darolutamide is not approved by the U.S. FDA, the European Medicines Agency or any other health authority.

About castration-resistant prostate cancer (CRPC)

Prostate cancer is the second most commonly diagnosed malignancy in men worldwide.2 In 2018, an estimated 1.2 million men were diagnosed with prostate cancer, and about 358,000 died from the disease worldwide.2 Prostate cancer is the fifth leading cause of death from cancer in men.2 Prostate cancer results from the abnormal proliferation of cells within the prostate gland, which is part of a man’s reproductive system.3 It mainly affects men over the age of 50, and the risk increases with age.4 Treatment options range from surgery to radiation treatment to therapy using hormone-receptor antagonists, i.e., substances that stop the formation of testosterone or prevent its effect at the target location.5 However, in nearly all cases, the cancer eventually becomes resistant to conventional hormone therapy.6

CRPC is an advanced form of the disease where the cancer keeps progressing even when the amount of testosterone is reduced to very low levels in the body. The field of treatment options for castration-resistant patients is evolving rapidly, but until recently, there have been no effective treatment options for CRPC patients who have rising prostate-specific antigen (PSA) levels while on ADT and no detectable metastases. In men with progressive nmCRPC, a short PSA doubling time has been consistently associated with reduced time to first metastasis and death.7

Aduro Biotech Reports Fourth Quarter and Full Year 2018 Financial Results

On February 27, 2019 Aduro Biotech, Inc. (NASDAQ: ADRO) reported financial results for the fourth quarter and full year ended December 31, 2018 (Press release, Aduro Biotech, FEB 27, 2019, View Source;p=RssLanding&cat=news&id=2389321 [SID1234533779]).

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"2018 was an important year for Aduro as we prioritized our core technologies and determined a go-forward strategy that is committed to maintaining a leadership role in the STING and APRIL pathways and advancing our clinical programs in areas of high unmet medical need," said Stephen T. Isaacs, chairman, president and chief executive officer of Aduro. "With our strategic focus established and $277.9 million in cash taking us into 2022, we are eager to execute on our clinical development plans for 2019 and beyond."

Key Accomplishments in Fiscal Year 2018

STING

Presented first-in-human monotherapy clinical data for ADU-S100, a novel stimulator of interferon genes (STING) pathway activator, and preliminary observations of ADU-S100 in combination with spartalizumab during the Society for Immunotherapy of Cancer (SITC) (Free SITC Whitepaper)’s (SITC) (Free SITC Whitepaper) 33rd Annual Meeting
Entered into a research collaboration and exclusive license agreement with Eli Lilly and Company (Lilly) for the cGAS-STING pathway inhibitor program for autoimmune and inflammatory diseases
Presented preclinical data on the role of intratumoral STING activation by ADU-S100 in combination with checkpoint inhibitors in anti-tumor immunity at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2018 and the SITC (Free SITC Whitepaper) 33rd Annual Meeting
Published a paper titled, "Magnitude of Therapeutic STING Activation Determines CD8+ T-Cell Mediated Anti-Tumor Immunity," in the peer-reviewed journal, Cell Reports
APRIL

Presented preclinical data on BION-1301 for the treatment of IgA nephropathy at the American Society of Nephrology (ASN) Kidney Week 2018
Presented preclinical data on BION-1301 for the treatment of multiple myeloma at the AACR (Free AACR Whitepaper) Annual Meeting 2018 and 60th American Society of Hematology (ASH) (Free ASH Whitepaper) Annual Meeting and Exposition
Published a paper titled, "APRIL signaling via TACI mediates immunosuppression by T regulatory cells in multiple myeloma: therapeutic implications," in the peer-reviewed journal, Leukemia
Financial Results

Cash Position – Cash, cash equivalents and marketable securities totaled $277.9 million at December 31, 2018, compared to $349.7 million at December 31, 2017. In the fourth quarter of 2018, Aduro collected an $18.1 million cash tax refund from the Internal Revenue Service related to its carryback claim for 2017 losses.

Revenue – Revenues were $2.8 million for the fourth quarter of 2018 and $15.1 million for the full year 2018, compared to $3.8 million and $17.2 million, respectively, for the same periods in 2017. The decrease in revenue in both periods was primarily due to the adoption of the ASC 606 accounting standard on January 1, 2018, which resulted in a change in revenue recognition methodology under our Novartis collaboration agreement.

Expenses – Research and development expenses were $17.6 million for the fourth quarter of 2018 and $75.8 million for the full year 2018, compared to $22.9 million and $89.4 million, respectively, for the same periods in 2017. The decrease in research and development expenses for both periods was primarily due to lower expenses for our antibody and LADD programs.

General and administrative expenses were $9.0 million for the fourth quarter of 2018 and $36.0 million for the full year 2018, compared to $8.8 million and $33.8 million, respectively, for the same periods in 2017. The increase in general and administrative expenses for both periods was primarily due to higher professional services and consulting costs as well as stock-based compensation expense.

Loss on impairment of intangible assets was $4.0 million for the fourth quarter and full year 2018. This expense was recorded due to the discontinuation of one of our acquired early research programs.

Net Loss – Net loss for the fourth quarter and year ended December 31, 2018 was $26.3 million, or $0.33 per share, and $95.4 million, or $1.21 per share, respectively. This compared to net loss of $26.1 million, or $0.34 per share, and $91.9 million, or $1.26 per share, respectively, for the same periods in 2017. The increase in net loss for the year was primarily due to the income tax benefit recorded in 2017.

Calithera Biosciences Announces CB-708 Preclinical Data Presentation at the AACR Annual Meeting
2019

On February 27, 2019 Calithera Biosciences, Inc. (Nasdaq: CALA), a clinical stage biotechnology company focused on discovering and developing novel small molecule drugs for the treatment of cancer and other life-threatening diseases, reported that preclinical data highlighting the potential of CB-708, the company’s orally bioavailable CD73 inhibitor will be presented in a poster session at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2019, taking place March 29 to April 3, 2019 in Atlanta, Georgia (Press release, Calithera Biosciences, FEB 27, 2019, View Source [SID1234535228]).

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Details for the presentation are as follows:

Title: Reversal of adenosine-mediated immune suppression by CB-708, an orally bioavailable and potent small molecule inhibitor of CD73 Presenter:Clarissa Lee, Calithera Biosciences Session

Title: Novel Immunomodulatory Agents 2, Abstract #4134

Session Date and Time: Tuesday April 2, 20191:00 p.m. ET-5:00 p.m. ET

Location: Georgia World Congress Center, Exhibit Hall B, Poster Section 25, Board 8

Additional meeting information can be found at the AACR (Free AACR Whitepaper) website www.aacr.org.

The poster presentation will be available at www.calithera.com in the Publications Section.

CD73 is an enzyme in the tumor microenvironment that produces adenosine, a powerful inhibitor of immune function in tumors. CD73 is expressed across a wide range of tumor types and tumor infiltrating leukocytes. Expression of CD73 often correlates with poor prognosis in patients with cancer. Blockade of adenosine production by CD73 inhibition is expected to reverse immunosuppression in the tumor microenvironment and enhance the immune system’s ability to fight the cancer. CB-708 is an orally bioavailable small molecule inhibitor of CD73.

Madrigal Pharmaceuticals Reports 2018 Fourth Quarter and Full Year Financial Results and Highlights

On February 27, 2019 Madrigal Pharmaceuticals, Inc. (NASDAQ:MDGL) reported its fourth quarter and full year 2018 financial results and highlights (Press release, Synta Pharmaceuticals, FEB 27, 2019, View Source [SID1234533732]):

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"Madrigal made significant progress in 2018 in advancing the development of MGL-3196. We successfully completed Phase 2 studies in both NASH and dyslipidemia and expanded the Madrigal team to meet the demands of our clinical programs," stated Paul Friedman, M.D., Chief Executive Officer of Madrigal. "In June, we also raised approximately $312 million of net proceeds from a public offering of our common stock, and we believe we have significant financial resources to fund our currently planned Phase 3 programs."

Becky Taub, M.D., CMO and Executive VP, Research & Development of Madrigal added, "We had a positive end of phase 2 meeting with FDA for our NASH program, and we expect to initiate our Phase 3 clinical trial before the end of the first quarter of 2019. We continue to believe MGL-3196 has the potential to resolve NASH while decreasing cardiovascular risk, through reduction of levels of multiple atherogenic lipids as well as reduction of fat in the liver. Based on this potential cardiovascular risk reducing profile, we also intend to move ahead with our Phase 3 dyslipidemia clinical program later this year."

Financial Results for the Three Months and Twelve Months Ended December 31, 2018

As of December 31, 2018, Madrigal had cash, cash equivalents and marketable securities of $483.7 million, compared to $191.5 million at December 31, 2017. The increase in cash and marketable securities resulted primarily from the net proceeds of $311.8 million from Madrigal’s public offering of common stock in June 2018, partially offset by cash used in operations of $25.5 million.

Operating expenses were $14.5 million and $40.7 million, respectively, for the three month and twelve month periods ended December 31, 2018, compared to $8.9 million and $32.1 million in the comparable prior year periods.

Research and development expenses for the three month and twelve month periods ended December 31, 2018 were $8.9 million and $25.4 million, respectively, compared to $6.5 million and $24.4 million in the comparable prior year periods. The increases are primarily attributable to increases in non-cash stock compensation, personnel and

consulting costs, the effects of which were partially offset by lower clinical costs due to completion of treatment in our Phase 2 clinical studies in 2018.

General and administrative expenses for the three month and twelve month periods ended December 31, 2018 were $5.6 million and $15.3 million, respectively, compared to $2.4 million and $7.7 million in the comparable prior year periods. The increases are due primarily to higher non-cash stock compensation expense from stock option awards.

Interest income for the three month and twelve month periods ended December 31, 2018 was $3.0 million and $7.7 million, respectively, as compared to $216 thousand and $558 thousand in the comparable prior year periods. The change in interest income was due primarily to a higher average principal balance in our investment account in 2018, and increased interest rates.

Clinical Program Summaries for MGL-3196

NASH

Non-alcoholic Steatohepatitis (NASH) is a common liver disease in the United States and worldwide, unrelated to alcohol use, that is characterized by a build-up of fat in the liver, inflammation, damage (ballooning) of hepatocytes and increasing fibrosis. Although people with NASH may feel well and often do not know they have the disease, NASH can lead to permanent damage, including cirrhosis and impaired liver function in a high percentage of patients.

In October 2016, the first patient was treated in the ongoing Phase 2 trial of MGL-3196 for the treatment of NASH. The randomized, double-blind, placebo-controlled, multi-center Phase 2 study enrolled 125 patients 18 years of age and older with liver biopsy-confirmed NASH and included approximately 25 clinical sites in the United States. Patients were randomized to receive either MGL-3196 or placebo in a 2:1 ratio.

The primary endpoint of the study was the reduction of liver fat at 12 weeks compared with baseline (relative change), assessed by MRI-PDFF. Key secondary endpoints at 36 weeks included: reduction in liver fat compared with baseline (relative change), also assessed by MRI-PDFF; a two-point reduction in NAS (NALFD activity score) on biopsy; resolution of NASH on biopsy; and, safety and tolerability based on adverse events and changes in laboratory values.

The primary endpoint of the study at 12 weeks was achieved. Liver fat was reduced by 36.3% in all MGL-3196 treated patients (78) and 42.0% in a pre-specified group of high exposure MGL-3196 treated patients (44/78), as compared with 9.6% median reduction in liver fat in 38 placebo treated patients. These results were statistically significant (p<0.0001) for both MGL-3196 treatment groups. Further, 75% of the high-exposure MGL-3196 treated patients showed liver fat reductions of >30%.

At 36 weeks, MGL-3196 achieved multiple key secondary endpoints including a sustained highly significant (p<0.001) reduction in liver fat compared to placebo as measured by MRI-PDFF; mean relative fat reduction for MGL-3196 was 37% versus 8.9% for placebo. MGL-3196 was associated with a greater percentage of subjects with a 2-point improvement in NAS (56% of 73 patients vs 32% of 34 placebo subjects, p=0.02). NASH resolution (NR) was seen in 27% of MGL-3196 compared with 6% of placebo subjects, p=0.02. MGL-3196 patients with > 30% fat reduction on Week 12 MRI-PDFF demonstrated a higher percentage of 2-point improvement in NAS (70%, p=0.001) and NR (39%, p=0.001) compared with placebo, demonstrating a strong relationship between early reduction in liver fat as demonstrated by week 12 MRI-PDFF and NASH improvement on liver biopsy at Week 36. In patients with NASH Resolution, 35% of the MGL-3196 treated patients and no placebo patients had more advanced NASH (baseline NAS >5).

At Week 36, MGL-3196 treated patients showed sustained reduction of fibrosis biomarkers. In MGL-3196 patients with NASH resolution, fibrosis also resolved in 50% of patients and was decreased statistically significantly relative to all placebo patients.

There were statistically significant reductions in liver enzymes in MGL-3196 treated patients compared to placebo treated patients; reductions of greater magnitude were achieved with longer duration of MGL-3196 treatment. Statistically significantly more MGL-3196 treated patients than placebo treated patients had normalization of ALT (alanine transaminase).

Similar to week 12, at week 36 there were sustained, statistically significant reductions in low-density lipoprotein cholesterol (LDL-C), triglycerides, ApoB and lipoprotein(a).

MGL-3196 was well tolerated in this trial with mostly mild and a few moderate AEs which were balanced between drug treated and placebo patients. There was an increase in incidence of mild transient diarrhea in MGL-3196-treated, often a single episode, at the start of treatment. Diarrhea incidence was not increased later in the study.

Based on liver enzyme inclusion criteria, some patients are receiving extended treatment beyond 36 weeks for up to 36 additional weeks. All patients in this extension study will receive MGL-3196 and only non-invasive assessments will be made, including serial MRI-PDFF, safety labs, and circulating biomarkers.

Additional information about the study [NCT02912260] can be obtained at www.ClinicalTrials.gov.

Dyslipidemia

Patients with NASH, and its more prevalent precursor, Non-Alcoholic Fatty Liver Disease (NAFLD), are at heightened cardiovascular risk. In fact, patients suffering from these conditions die more frequently from cardiovascular events than from their liver

disease. Multiple factors may contribute to this risk, including elevated levels of LDL-C and excess liver fat. Patients with NASH and NAFLD, however, may not undergo a biopsy to confirm a NASH diagnosis until they reach the more advanced stages of fibrosis (F2 — F4). A significant segment of this large group of patients may also suffer from diabetes and metabolic syndrome, and have lipid levels that are above target despite treatment with established therapies. These patients may benefit from therapy to lower their lipid levels, including excess liver fat.

We believe Madrigal’s studies to date in patients with NASH and patients with heterozygous familial hypercholesterolemia (HeFH), have demonstrated the pleiotropic activity of MGL-3196 and the potential of the drug to reduce an array of atherogenic lipids, including liver fat, LDL-C, ApoB, triglycerides, ApoCIII, and Lp(a), as well as hs-CRP. As a result, Madrigal intends to focus its development of MGL-3196 for the treatment of patients across the entire NASH and NAFLD spectrum.

HeFH
Heterozygous familial hypercholesterolemia (HeFH), and a much rarer form called homozygous familial hypercholesterolemia (HoFH), are severe genetic dyslipidemias typically caused by inactivating mutations in the LDL receptor. Both forms of FH lead to early onset cardiovascular disease. HeFH, the most common dominantly inherited disease, is present in up to 1 in 200 people; the disease is found in higher frequencies in certain more genetically homogenous populations. Treatments exist for both HeFH and HoFH but many patients (as many as 40 percent of HeFH patients) are not able to reach their cholesterol (LDL-C) reduction goals on these therapies, reflecting the lifetime burden of cholesterol buildup in their bodies. Based on evidence of impressive LDL cholesterol lowering in Phase 1, and data suggesting that MGL-3196 has a mechanism of action that is different from and complementary to statins, Madrigal initiated a Phase 2 proof-of-concept trial in HeFH in February 2017 and enrolled 116 patients.

In this Phase 2 HeFH trial, patients who were not at their LDL-C goal were randomized in a 2:1 ratio to receive either MGL-3196 or placebo, in addition to their current cholesterol lowering regimen, which included approximately 75% taking high intensity statins (20/40 mg rosuvastatin or 80 mg atorvastatin), and about 2/3 of patients also taking ezetimibe. MGL-3196 treated patients (placebo corrected) achieved highly significant (p< 0.0001) LDL-C lowering of 18.8%, and 21% LDL-C lowering in those on an optimal dose of MGL-3196. LDL-C lowering was 28.5% in MGL-3196 treated compared to placebo in a prespecified group of patients who did not tolerate high intensity statin doses. Highly significant reductions (p<0.0001) relative to placebo were also observed with ApoB, triglycerides (TG) (25-31%), apolipoprotein CIII (Apo CIII) and Lp(a) (25-40%) in all MGL-3196 treated patients and prespecified subgroups, irrespective of statin treatment.

MGL-3196 was well-tolerated with primarily mild and some moderate AEs, the numbers of which were balanced between placebo and drug-treatment groups.

About MGL-3196

Among its many functions in the human body, thyroid hormone, through activation of its beta receptor, plays a central role in controlling lipid metabolism, impacting a range of health parameters from levels of serum cholesterol and triglycerides to the pathological buildup of fat in the liver. Attempts to exploit this pathway for therapeutic purposes in cardio-metabolic and liver diseases have been hampered by the lack of selectivity of older compounds for the thyroid hormone receptor (THR)-β, chemically-related toxicities and undesirable distribution in the body.

Madrigal recognized that greater selectivity for thyroid hormone receptor (THR)-β and liver targeting might overcome these challenges and deliver the full therapeutic potential of THR-β agonism. Madrigal believes that MGL-3196 is the first orally administered, small-molecule, liver- directed, truly β-selective THR agonist. MGL- 3196 has now demonstrated in two Phase 2 double-blind, placebo-controlled trials in NASH and HeFH the potential for a broad array of therapeutically beneficial effects, improving components of both metabolic syndrome, such as insulin resistance and dyslipidemia, and fatty liver disease, including lipotoxicity and inflammation. Based on evidence of these pleiotropic actions, coupled with an excellent safety profile, Madrigal plans to initiate a Phase 3 clinical program in NASH, and a Phase 3 clinical program is dyslipidemia

Alpine Immune Sciences to Present at Two Upcoming Investor Conferences

On February 27, 2019 Alpine Immune Sciences, Inc. (NASDAQ:ALPN), a leading clinical-stage immunotherapy company focused on developing innovative treatments for cancer, autoimmune/inflammatory, and other diseases, reported the company will participate in two upcoming investor conferences in March (Press release, Alpine Immune Sciences, FEB 27, 2019, View Source [SID1234533748]).

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Cowen and Company 39th Annual Health Care Conference
Date: Tuesday, March 12, 2019
Time: 9:20 a.m. Eastern Time
Location: Boston, MA

Oppenheimer 29th Annual Healthcare Conference – Analyst-Led Fireside Chat
Date: Tuesday, March 19, 2019
Time: 1:35 p.m. Eastern Time
Location: New York, NY

A live webcast of each presentation will be available online in the investor relations section of the company’s website at View Source A replay of the presentations will be available on the company website for 90 days following the webcast.