Propanc Biopharma Receives Expression of Interest to Evaluate Proenzyme Therapy in Pancreatic and Ovarian Cancer Patients

On January 18, 2021 Propanc Biopharma, Inc. (OTC: PPCB) ("Propanc" or the "Company"), a biopharmaceutical company developing novel cancer treatments for patients suffering from recurring and metastatic cancer, reported that the Company has received expressions of interest to evaluate proenzyme therapy as a method to prevent recurrence and metastasis of solid tumors in pancreatic and ovarian cancers (Press release, Propanc, JAN 18, 2021, View Source [SID1234574079]). The letters of interest were confirmed by Drs Natalia Luque Caro and Fernando Gálvez Montosa, medical oncologists specializing in pancreatic and ovarian cancers, respectively, from the University Hospital of Jaén, in Granada, Spain. The evaluation will most likely be conducted as separate Phase IIa proof of concept (POC), multi-trial center studies for each target indication.

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The expressions of interest were confirmed after evaluation of Propanc’s scientific literature supporting the use of proenzymes in pancreatic and ovarian cancers. The Phase IIa POC studies will be conducted after a Phase Ib dose escalation study evaluating the tolerability and activity of proenzyme therapy in patients with advanced solid tumors is completed, planned for 2021, at the Peter Mac Cancer Center, Melbourne, Australia.

"Receiving expressions of interest from Drs Caro and Montoya at the University Hospital of Jaén provides important infrastructure to plan our multi-trial center studies, which will likely require up to 60 patients for each study in pancreatic and ovarian cancers, which is why we were thinking of running these trials in Europe, due to the larger patient populations," said James Nathanielsz, Propanc’s Chief Executive Officer. "By running multi-trial centre studies for our Phase IIa studies, we ensure that we have sufficient numbers to complete the trials more efficiently than if we ran the trials in Australia, alone. Furthermore, the University Hospital of Jaén is located in Granada, Spain, and is a well-known biopharmaceutical hub with a strong reputation among multi-national companies. We look forward to a potential collaboration with the clinical trial investigators from this reputable institution."

Enhertu approved in the US for the treatment of patients with previously treated HER2-positive advanced gastric cancer

On January 18, 2021 AstraZeneca and Daiichi Sankyo Company, Limited (Daiichi Sankyo)’s Enhertu (trastuzumab deruxtecan) reported that it has been approved in the US for the treatment of adult patients with locally advanced or metastatic HER2-positive gastric or gastroesophageal junction (GEJ) adenocarcinoma who have received a prior trastuzumab-based regimen (Press release, AstraZeneca, JAN 18, 2021, View Source [SID1234574074]).

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In the US, gastric cancer is most frequently diagnosed in the advanced stage, with only approximately 5% of patients surviving beyond five years.1,2 Approximately one in five gastric cancers are HER2 positive.3

The approval by the Food and Drug Administration (FDA) was based on the positive results from the randomised DESTINY-Gastric01 Phase II trial conducted in Japan and South Korea. In the trial, Enhertu demonstrated a statistically significant and clinically meaningful improvement in overall survival (OS) and objective response rate (ORR) versus chemotherapy (irinotecan or paclitaxel) in patients with advanced gastric cancer or GEJ adenocarcinoma who had progressed on at least two or more prior regimens including trastuzumab plus a fluoropyrimidine- and platinum-based chemotherapy combination.4

Ronan Kelly, MD, MBA, Director of the Charles A. Sammons Cancer Center and the W.W. Caruth, Jr. Chair of Immunology at Baylor University Medical Center, Dallas, Texas, US, said: "Patients with metastatic HER2-positive gastric cancer with progression following 1st-line treatment have historically faced poor outcomes, including low response to treatment and rapid disease progression. This approval represents the first time a HER2-directed medicine has demonstrated a significant improvement in survival compared to chemotherapy following initial treatment in the metastatic setting, and it has the potential to become the new standard of care for this patient population."

Dave Fredrickson, Executive Vice President, Oncology Business Unit, said: "Today’s approval of Enhertu represents the first HER2-directed medicine approved in a decade for patients with HER2-positive metastatic gastric cancer. The results from the DESTINY-Gastric01 trial highlight the potential to change clinical practice, showing a 41 per cent improvement in survival and a response rate more than three times higher with Enhertu compared to chemotherapy. We are thrilled to bring this important medicine to more patients and physicians in the US."

Antoine Yver, Executive Vice President and Global Head, Oncology Research and Development, Daiichi Sankyo, said: "Enhertu is the first antibody drug conjugate to receive approval in the US for the treatment of patients with metastatic gastric cancer, and represents a major advance in managing this difficult-to-treat disease. This second indication in the US represents an important step forward in our ambitious plan to accelerate the development of Enhertu across a broad range of HER2-targetable cancers."

In a pre-specified interim analysis from the DESTINY-Gastric01 trial, patients treated with Enhertu had a 41% reduction in the risk of death versus patients treated with chemotherapy (based on a hazard ratio [HR] of 0.59; 95% confidence interval [CI] 0.39-0.88; p=0.0097) with a median OS of 12.5 months versus 8.4 months.3

Confirmed ORR, assessed by independent central review was a major efficacy outcome. Results showed a confirmed ORR of 40.5% in patients treated with Enhertu (n=126) compared to 11.3% in patients treated with chemotherapy (n=62). Patients treated with Enhertu had a 7.9% complete response rate and a 32.5% partial response rate compared to a complete response rate of 0% and a partial response rate of 11.3% for patients treated with chemotherapy.4

Enhertu demonstrated a median progression-free survival (PFS) of 5.6 months compared to 3.5 months with chemotherapy (HR=0.47; 95% CI 0.31-0.71). Additionally, Enhertu showed a median duration of response (DoR) of 11.3 months versus 3.9 months with chemotherapy.4

Results from the DESTINY-Gastric01 trial were published in The New England Journal of Medicine in June 2020.5

The most common adverse reactions, including laboratory abnormalities, of any grade (greater than or equal to 20%) for patients treated with Enhertu (n=125) in the DESTINY-Gastric01 trial were anaemia, leukopenia, neutropenia, lymphocytopenia, thrombocytopenia, nausea, decreased appetite, increased aspartate aminotransferase, fatigue, increased blood alkaline phosphatase, increased alanine aminotransferase, diarrhoea, hypokalaemia, vomiting, constipation, increased blood bilirubin, pyrexia and alopecia. Interstitial lung disease or pneumonitis occurred in 10% of patients.4

This is the second indication approved for Enhertu in the US following the accelerated approval for adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting based on the DESTINY-Breast01 trial.

Enhertu was previously granted Priority Review, Breakthrough Therapy Designation (BTD) in HER2-positive metastatic gastric cancer and Orphan Drug Designation for gastric cancer by the FDA. Two additional Phase II trials, DESTINY-Gastric02 and DESTINY-Gastric03, are underway, further evaluating treatment with Enhertu in patients with HER2-positive metastatic gastric cancer.

Financial considerations
Following US approval, an amount of $115m is due from AstraZeneca to Daiichi Sankyo as a combined 2nd-line and 3rd-line milestone payment in HER2-positive gastric cancer. In AstraZeneca, the milestones paid will be capitalised as an addition to the upfront payment made in 2019 and subsequent capitalised milestones and amortised through the profit and loss.

Sales of Enhertu in the US are recognised by Daiichi Sankyo. AstraZeneca reports its share of gross profit margin from Enhertu sales in the US as collaboration revenue in the Company’s financial statements. For further details on the financial arrangements, please consult the collaboration agreement from March 2019.

Gastric cancer
Gastric (stomach) cancer is the fifth most common cancer worldwide and the third leading cause of cancer mortality with a five-year survival rate of 5% for metastatic disease; there were approximately one million new cases reported in 2020 and more than 768,000 deaths.6 In the US, it is estimated that 27,600 new cases of gastric cancer were diagnosed in 2020 and more than 11,000 people died from the disease.7

Approximately one in five gastric cancers are HER2 positive.1 HER2 is a tyrosine kinase receptor growth-promoting protein expressed on the surface of many types of tumours including breast, gastric, lung and colorectal cancers. Gastric cancer is usually diagnosed in the advanced stage, but even when diagnosed in earlier stages of the disease the survival rate remains modest.2 Recommended 1st-line treatment for HER2-positive advanced or metastatic gastric cancer is combination chemotherapy plus trastuzumab, an anti-HER2 medicine, which has been shown to improve survival outcomes when added to chemotherapy. For patients with metastatic gastric cancer that progresses following initial treatment with a trastuzumab-based regimen, there were previously no other approved HER2-targeted medicines prior to the approval of Enhertu.8

DESTINY-Gastric01
DESTINY-Gastric01 is a Phase II, open-label, multi-centre, randomised controlled trial testing the safety and efficacy of Enhertu (6.4 mg/kg) versus investigator’s choice of chemotherapy in a primary cohort of patients from Japan and South Korea with HER2-positive (defined as IHC3+ or IHC2+/ISH+), locally advanced or metastatic gastric cancer or GEJ adenocarcinoma who have progressed on at least two or more prior regimens including trastuzumab plus a fluoropyrimidine- and platinum-based chemotherapy combination. Patients (n=188) were randomised 2:1 to receive Enhertu or physician’s choice of chemotherapy (paclitaxel or irinotecan monotherapy). Patients were treated with Enhertu 6.4mg/kg once every three weeks or chemotherapy.

The main efficacy outcome measures were ORR, assessed by independent central review, and OS. Additional efficacy outcome measures were PFS and DoR.4

Enhertu
Enhertu (trastuzumab deruxtecan; fam-trastuzuab deruxtecan-nxki in the US) is a HER2-directed antibody drug conjugate (ADC). It is the lead ADC in the oncology portfolio of Daiichi Sankyo and the most advanced programme in AstraZeneca’s ADC scientific platform.

ADCs are targeted cancer medicines that deliver cytotoxic chemotherapy (‘payload’) to cancer cells via a linker attached to a monoclonal antibody that binds to a specific target expressed on cancer cells. Enhertu is comprised of a humanised anti-HER2 IgG1 monoclonal antibody with the same amino acid sequence as trastuzumab attached to a topoisomerase I inhibitor payload, an exatecan derivative, via a tetrapeptide-based cleavable linker.

Enhertu (5.4mg/kg) is approved in the US under accelerated approval, and in Japan under the conditional early approval system, for the treatment of adult patients with unresectable or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2-based regimens in the metastatic setting based on the DESTINY-Breast01 trial. In addition to the US, Enhertu (6.4mg/kg) is also approved in Japan for patients with HER2-positive unresectable advanced or recurrent gastric cancer that progressed after chemotherapy based on the DESTINY-Gastric01 trial.

Development programme
A comprehensive development programme is underway globally, with nine registrational trials evaluating the efficacy and safety of Enhertu monotherapy across multiple HER2 cancers, including breast, gastric and lung cancers. Trials in combination with other anticancer treatments, such as immunotherapy, are also underway.

In May 2020, Enhertu received a BTD for the treatment of patients with metastatic non-small cell lung cancer whose tumours have a HER2 mutation and with disease progression on or after platinum-based therapy.

Daiichi Sankyo collaboration
Daiichi Sankyo and AstraZeneca entered into a global collaboration to jointly develop and commercialise Enhertu (a HER2-directed ADC) in March 2019, and datopotamab deruxtecan (a TROP2-directed ADC) in July 2020, except in Japan where Daiichi Sankyo maintains exclusive rights. Daiichi Sankyo is responsible for manufacturing and supply of Enhertu and datopotamab deruxtecan.

AstraZeneca in gastrointestinal cancers
AstraZeneca has a broad development programme for the treatment of gastrointestinal (GI) cancers across several medicines spanning a variety of tumour types and stages of disease. In 2020, GI cancers collectively represented over five million new cancer cases leading to more than 3.5 million deaths.6 Within this programme, the Company is committed to improving outcomes in gastric, liver, oesophageal, pancreatic, and colorectal cancers.

The Company aims to understand the potential of Enhertu in the two most common GI cancers, colorectal and gastric cancers. Imfinzi (durvalumab) is being assessed as both as monotherapy and in combinations including with tremelimumab across the two main types of liver cancer, hepatocellular carcinoma and biliary tract cancer, and in oesophageal and gastric cancers. Lynparza (olaparib) is a first-in-class PARP inhibitor with a broad and advanced clinical trial programme across multiple GI tumour types including pancreatic and colorectal cancers. Lynparza is developed and commercialised in collaboration with MSD (Merck & Co., Inc. inside the US and Canada).

AstraZeneca in oncology
AstraZeneca has a deep-rooted heritage in oncology and offers a quickly growing portfolio of new medicines that has the potential to transform patients’ lives and the Company’s future. With seven new medicines launched between 2014 and 2020, and a broad pipeline of small molecules and biologics in development, the Company is committed to advance oncology as a key growth driver for AstraZeneca focused on lung, ovarian, breast and blood cancers.

By harnessing the power of six scientific platforms – Immuno-Oncology, Tumour Drivers and Resistance, DNA Damage Response, Antibody Drug Conjugates, Epigenetics, and Cell Therapies – and by championing the development of personalised combinations, AstraZeneca has the vision to redefine cancer treatment and, one day, eliminate cancer as a cause of death.

Sirnaomics Announces First Patient Dosed In Phase 2a Study of STP705 for Treatment of Cutaneous Basal Cell Carcinoma, Company Expects to Report Initial Clinical Data in 2021

On January 17, 2021 Sirnaomics, Inc., a biopharmaceutical company engaged in the discovery and development of RNAi therapeutics against cancer and fibrotic diseases, reported dose administration for the first patient in a Phase 2a clinical study of the company’s lead drug candidate, STP705, for the treatment of cutaneous basal cell carcinoma (Press release, Sirnaomics, JAN 17, 2021, View Source [SID1234574527]).

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The open label, dose escalation study is designed to evaluate the efficacy and safety of intralesional injection of STP705 in adult patients with cutaneous basal cell carcinoma confirmed with biopsy samples. The objective is to determine the safe and effective recommended dose of STP705 for the treatment of basal cell carcinoma (BCC), as well as analysis of biomarkers common to BCC formation pathway including TGF-β1 and COX-2. The trial is comprised of three dose escalation cohorts ranging from 30 μg to 90 μg with five patients in each group, and a total of 15 patients will be enrolled in the trial. Participants will receive injections of STP705 once a week for up to six weeks.

Bcc Pic1
The primary endpoint of this trial is to evaluate patients for complete histological clearance of the tumor cells within the treated BCC lesion with secondary endpoints, evaluating subjects for investigational product treatment related adverse events, as well as serious adverse events, and cutaneous skin reactions.

"This marks another significant milestone as we continue to leverage our polypeptide nano-particle technology for siRNA drug delivery to advance our pipeline of oncology therapeutic candidates," said Patrick Lu, Ph.D., the founder, President and CEO of Sirnaomics. "We look forward to obtaining important clinical readouts in this trial and increasing the probability of success, while continuing to demonstrate our leadership in RNAi therapeutic development for skin cancers."

"This is an important study and milestone for Sirnaomics, the STP705 program, and potentially for patients with BCC, as it could offer an alternative to surgical excision of these lesions," said Michael Molyneaux M.D., Chief Medical Officer. "The company recognizes that there is a high unmet need for non-surgical treatments for various types of nonmelanoma skin cancers that reduce scarring and achieve high rates of histological clearance."

The Company expects to report initial clinical data from the trial in 2021.

Additional information about this clinical trial is available at clinicaltrials.gov using the identifier: NCT04669808.

About Basal Cell Carcinoma

Basal cell carcinoma (BCC) is a type of nonmelanoma skin cancer that occurs most often on areas that are exposed to the sun, such as head and neck. The most commonly found clinical feature of BCC is an elevated tumor with a pearly and translucent margin and telangiectasia. The color may vary widely from nearly normal skin color to erythematous to violaceous and may also be pigmented. BCC may also resemble noncancerous skin conditions such as eczema or psoriasis. The majority of these cancers occur on areas of skin that are regularly exposed to sunlight or other ultraviolet radiation. It is believed that development of BCC is linked closely to overexpression of TGF-β1 and COX-2.

Surgery is the currently the most common treatment option for the treatment of nonmelanoma cancer. The various forms of surgical modalities carry significant cutaneous adverse events, risk of scar, infection and bleeding. Surgery can also have a significant recurrence rate. As a result, there is a high unmet need for an FDA approved local injection therapy that is safe and effective.

Bcc Pic2
About STP705
Sirnaomics’ leading product candidate, STP705, is a siRNA (small interfering RNA) therapeutic that takes advantage of a dual-targeted inhibitory property and polypeptide nanoparticle (PNP)-enhanced delivery to directly knock down both TGF-β1 and COX-2 gene expression. The product candidate has received multiple IND approvals from both the US FDA and Chinese NMPA, including treatments of cholangiocarcinoma, nonmelanoma skin cancer and hypertrophic scar. STP705 has also received Orphan Drug Designation for treatment of cholangiocarcinoma and primary sclerosing cholangitis. Preclinical animal models using STP705 have demonstrated a dramatic improvement in T-cell penetration into tumors in the liver with single agent action as well as improvement in the efficacy of an anti-PD-L1 antibody checkpoint inhibitor in an HCC model. This effect may improve other immune checkpoint inhibitor efficacies in addition to those targeting the PD-1/PD-L1 axis.

Sirnaomics Announces First Patient Dosed In Phase 2a Study of STP705 for Treatment of Cutaneous Basal Cell Carcinoma

On January 17, 2021 Sirnaomics, Inc., a biopharmaceutical company engaged in the discovery and development of RNAi therapeutics against cancer and fibrotic diseases, reported dose administration for the first patient in a Phase 2a clinical study of the company’s lead drug candidate, STP705, for the treatment of cutaneous basal cell carcinoma (Press release, Sirnaomics, JAN 17, 2021, View Source [SID1234574073]).

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The open label, dose escalation study is designed to evaluate the efficacy and safety of intralesional injection of STP705 in adult patients with cutaneous basal cell carcinoma confirmed with biopsy samples. The objective is to determine the safe and effective recommended dose of STP705 for the treatment of basal cell carcinoma (BCC), as well as analysis of biomarkers common to BCC formation pathway including TGF-β1 and COX-2. The trial is comprised of three dose escalation cohorts ranging from 30 μg to 90 μg with five patients in each group, and a total of 15 patients will be enrolled in the trial. Participants will receive injections of STP705 once a week for up to six weeks.

The primary endpoint of this trial is to evaluate patients for complete histological clearance of the tumor cells within the treated BCC lesion with secondary endpoints, evaluating subjects for investigational product treatment related adverse events, as well as serious adverse events, and cutaneous skin reactions.

"This marks another significant milestone as we continue to leverage our polypeptide nano-particle technology for siRNA drug delivery to advance our pipeline of oncology therapeutic candidates," said Patrick Lu, Ph.D., the founder, President and CEO of Sirnaomics. "We look forward to obtaining important clinical readouts in this trial and increasing the probability of success, while continuing to demonstrate our leadership in RNAi therapeutic development for skin cancers."

"This is an important study and milestone for Sirnaomics, the STP705 program, and potentially for patients with BCC, as it could offer an alternative to surgical excision of these lesions," said Michael Molyneaux M.D., Chief Medical Officer. "The company recognizes that there is a high unmet need for non-surgical treatments for various types of nonmelanoma skin cancers that reduce scarring and achieve high rates of histological clearance."

The Company expects to report initial clinical data from the trial in 2021.

Additional information about this clinical trial is available at clinicaltrials.gov using the identifier: NCT04669808.

About Basal Cell Carcinoma
Basal cell carcinoma (BCC) is a type of nonmelanoma skin cancer that occurs most often on areas that are exposed to the sun, such as head and neck. The most commonly found clinical feature of BCC is an elevated tumor with a pearly and translucent margin and telangiectasia. The color may vary widely from nearly normal skin color to erythematous to violaceous and may also be pigmented. BCC may also resemble noncancerous skin conditions such as eczema or psoriasis. The majority of these cancers occur on areas of skin that are regularly exposed to sunlight or other ultraviolet radiation. It is believed that development of BCC is linked closely to overexpression of TGF-β1 and COX-2.

Surgery is the currently the most common treatment option for the treatment of nonmelanoma cancer. The various forms of surgical modalities carry significant cutaneous adverse events, risk of scar, infection and bleeding. Surgery can also have a significant recurrence rate. As a result, there is a high unmet need for an FDA approved local injection therapy that is safe and effective.

About STP705
Sirnaomics’ leading product candidate, STP705, is a siRNA (small interfering RNA) therapeutic that takes advantage of a dual-targeted inhibitory property and polypeptide nanoparticle (PNP)-enhanced delivery to directly knock down both TGF-β1 and COX-2 gene expression. The product candidate has received multiple IND approvals from both the US FDA and Chinese NMPA, including treatments of cholangiocarcinoma, nonmelanoma skin cancer and hypertrophic scar. STP705 has also received Orphan Drug Designation for treatment of cholangiocarcinoma and primary sclerosing cholangitis. Preclinical animal models using STP705 have demonstrated a dramatic improvement in T-cell penetration into tumors in the liver with single agent action as well as improvement in the efficacy of an anti-PD-L1 antibody checkpoint inhibitor in an HCC model. This effect may improve other immune checkpoint inhibitor efficacies in addition to those targeting the PD-1/PD-L1 axis.

Agios Presents Final Data from Phase 3 ClarIDHy Study of TIBSOVO® (ivosidenib tablets) in Patients with Previously Treated IDH1-Mutant Cholangiocarcinoma

On January 17, 2021Agios Pharmaceuticals, Inc. (NASDAQ:AGIO), a leader in the field of cellular metabolism to treat cancer and genetically defined diseases, today reported a full analysis of the final data, including mature overall survival (OS) results, from its global Phase 3 ClarIDHy trial of TIBSOVO (ivosidenib tablets) in patients with previously treated isocitrate dehydrogenase 1 (IDH1) mutated cholangiocarcinoma (Press release, Agios Pharmaceuticals, JAN 17, 2021, View Source [SID1234574070]). Data from the study were featured in an oral presentation at the American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) Gastrointestinal Cancers Symposium (ASCO-GI), which is being held virtually January 15-17, 2021.

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The final analysis showed an improvement in the secondary endpoint of OS favoring patients randomized to TIBSOVO compared to those randomized to placebo; however, statistical significance was not reached. The median OS for patients randomized to TIBSOVO was 10.3 months compared to 7.5 months for patients randomized to placebo (hazard ratio [HR]=0.79; 95% CI [0.56–1.12], 1-sided p=0.093). The protocol specified that patients randomized to placebo could cross over to TIBSOVO at the time of disease progression, and a high proportion of patients in the placebo arm (70.5%) crossed over to TIBSOVO. The results of a pre-specified analysis to adjust for crossover, based on the rank-preserving structural failure time (RPSFT) model, showed a median OS for patients in the placebo arm of 5.1 months (HR=0.49, 95% CI 0.34–0.70, 1-sided p<0.0001). The safety profile observed in the study was consistent with previously published data. As previously announced, the study demonstrated a statistically significant improvement in the primary endpoint of progression-free survival (PFS) by independent radiology review.

"The progression-free survival and overall survival data from the ClarIDHy Phase 3 study, coupled with a tolerable safety profile and supportive patient-reported quality-of-life data, demonstrate that TIBSOVO has the potential to be a clinically meaningful treatment option for patients with previously treated IDH1-mutant cholangiocarcinoma, an aggressive cancer with limited effective treatment options," said Andrew Zhu, M.D., Ph.D., director emeritus of liver cancer research at Massachusetts General Hospital, director of Jiahui International Cancer Center and professor of medicine at Harvard Medical School. "Treatment with TIBSOVO resulted in a consistent trend in improved overall survival, despite the high rate of crossover from the placebo arm, and this improvement was further supported by the pre-specified statistical analysis to adjust for the crossover effect. I look forward to the potential of having a new treatment option for my patients with this devastating disease."

"We are extremely pleased with the results of the ClarIDHy Phase 3 study, the first and only randomized Phase 3 trial for IDH1-mutant advanced cholangiocarcinoma, and believe TIBSOVO has demonstrated compelling results for patients facing a grim prognosis who currently have few treatment options," said Chris Bowden, M.D., chief medical officer at Agios. "We will collaborate closely with regulators to advance this potential new oral, non-cytotoxic, targeted treatment option, and we look forward to filing for U.S. approval later this quarter."

ClarIDHy Phase 3 Trial
The ClarIDHy trial is a global, randomized Phase 3 trial in previously treated IDH1-mutant cholangiocarcinoma patients who have documented disease progression following one or two systemic therapies in the advanced setting. Patients were randomized 2:1 to receive either single-agent TIBSOVO 500 mg once daily or placebo with crossover to TIBSOVO permitted at the time of documented radiographic progression per RECIST 1.1. The primary endpoint of the ClarIDHy trial is progression-free survival (PFS) as evaluated by independent radiology review. Secondary endpoints include investigator-evaluated PFS, safety and tolerability, overall response rate, OS, duration of response, pharmacokinetics, pharmacodynamics and quality of life assessments.

As of the May 31, 2020 data cutoff, 187 patients were randomized, with 126 patients in the TIBSOVO arm and 61 patients in the placebo arm. Forty-three patients randomized to placebo (70.5%) crossed over to open-label TIBSOVO upon radiographic disease progression and unblinding.

Updated Efficacy Data
Efficacy data as of the data cutoff showed:

The median OS for patients in the TIBSOVO arm was 10.3 months compared to 7.5 months for patients in the placebo arm (HR=0.79; 95% CI [0.56–1.12], 1-sided p=0.093).
After adjusting for crossover from placebo to TIBSOVO using the pre-specified analysis of rank-preserving structural failure time (RPSFT), the median OS for patients in the placebo arm was 5.1 months (HR=0.49; 95% CI [0.34–0.70], 1-sided p<0.0001).
The 6-month survival rate for patients in the TIBSOVO arm was 69 percent compared to 57 percent of patients in the placebo arm, not adjusted for crossover.
The 12-month survival rate for patients in the TIBSOVO arm was 43 percent compared to 36 percent for patients in the placebo arm, not adjusted for crossover.
Treatment with TIBSOVO preserved patients’ physical functioning from baseline, as assessed by the EORTC QLQ-C30 questionnaire, whereas patients in the placebo arm experienced decline from baseline at cycle 2, day 1 (2-sided p=0.002) and cycle 3, day 1 (2-sided p=0.004).
Treatment with TIBSOVO improved patients’ pain at cycle 2, day 1 compared to placebo, as assessed by the EORTC QLQ-BIL21 questionnaire (2-sided p=0.039); no difference was observed at cycle 3, day 1.
Neither arm was favored on other pre-specified quality-of-life subscales (QLQ-C30 Appetite Loss and QLQ-BIL21 Pain and Eating).
Updated Safety Data

Grade 3 or above treatment-emergent adverse events (TEAE) were reported in 53 percent of total TIBSOVO patients, which includes patients originally randomized to TIBSOVO and those who crossed over from placebo to TIBSOVO, compared to 37.3 percent of patients on placebo, with the most common being ascites (9.0% total TIBSOVO vs. 6.8% placebo), anemia (7.2% total TIBSOVO vs. 0% placebo) and increased blood bilirubin (5.4% total TIBSOVO vs. 1.7% placebo).
TEAEs leading to discontinuation were more common with placebo compared with total TIBSOVO (8.5% vs. 6.6%).
TEAEs leading to dose reductions (3.0% vs. 0%) and interruptions (30.1% vs. 18.6%) were more common with total TIBSOVO compared with placebo.
The most common TEAEs of any grade for total TIBSOVO were nausea (38.0%), diarrhea (33.1%) and fatigue (28.9%).
Previously Reported Data
Data from the study were previously presented at the European Society for Medical Oncology Congress (ESMO) (Free ESMO Whitepaper), held in September 2019 in Barcelona, Spain, and published in The Lancet Oncology on May 13, 2020. Results from the trial demonstrated a statistically significant improvement in the primary endpoint of PFS among patients randomized to TIBSOVO compared with placebo patients (HR=0.37; 95% CI [0.25–0.54], p<0.0001), with a median PFS of 2.7 months in the TIBSOVO arm versus a median PFS of 1.4 months in the placebo arm. The estimated PFS rate was 32 percent at six months and 22 percent at 12 months for patients randomized to TIBSOVO, while no patients randomized to placebo were free from progression or death beyond six months as of the data cut-off.

Based on these data, the National Comprehensive Cancer Network (NCCN) guidelines, the French National Treatment Guidelines for Biliary Cancer and the Italian Clinical Practice Guidelines on Cholangiocarcinoma were updated to recommend treatment with TIBSOVO for patients with advanced previously treated IDH1-mutant cholangiocarcinoma.

Agios plans to submit a supplemental new drug application for TIBSOVO in previously treated IDH1-mutant cholangiocarcinoma in the first quarter of 2021.

TIBSOVO is not approved in any country for the treatment of patients with previously treated advanced IDH1-mutant cholangiocarcinoma.

About Cholangiocarcinoma
Cholangiocarcinoma is a rare cancer of the bile ducts within and outside of the liver. Cases that occur within the liver are known as intrahepatic cholangiocarcinoma (IHCC) and those that occur outside the liver are considered extrahepatic. IDH1 mutations occur in approximately 10% of cholangiocarcinoma cases. Current treatment options for localized disease include surgery, radiation and/or other ablative treatments. There are no approved systemic therapies for IDH1-mutated cholangiocarcinoma and limited chemotherapy options are available in the advanced setting. Gemcitabine-based chemotherapy is often recommended for newly diagnosed advanced or metastatic disease.

About TIBSOVO (ivosidenib)
TIBSOVO is indicated for the treatment of acute myeloid leukemia (AML) with a susceptible isocitrate dehydrogenase-1 (IDH1) mutation as detected by an FDA-approved test in:

Adult patients with newly-diagnosed AML who are ≥75 years old or who have comorbidities that preclude use of intensive induction chemotherapy.
Adult patients with relapsed or refractory AML.
IMPORTANT SAFETY INFORMATION

WARNING: DIFFERENTIATION SYNDROME

Patients treated with TIBSOVO have experienced symptoms of differentiation syndrome, which can be fatal if not treated. Symptoms may include fever, dyspnea, hypoxia, pulmonary infiltrates, pleural or pericardial effusions, rapid weight gain or peripheral edema, hypotension, and hepatic, renal, or multi-organ dysfunction. If differentiation syndrome is suspected, initiate corticosteroid therapy and hemodynamic monitoring until symptom resolution.

WARNINGS AND PRECAUTIONS

Differentiation Syndrome: See Boxed WARNING. In the clinical trial, 25% (7/28) of patients with newly diagnosed AML and 19% (34/179) of patients with relapsed or refractory AML treated with TIBSOVO experienced differentiation syndrome. Differentiation syndrome is associated with rapid proliferation and differentiation of myeloid cells and may be life-threatening or fatal if not treated. Symptoms of differentiation syndrome in patients treated with TIBSOVO included noninfectious leukocytosis, peripheral edema, pyrexia, dyspnea, pleural effusion, hypotension, hypoxia, pulmonary edema, pneumonitis, pericardial effusion, rash, fluid overload, tumor lysis syndrome, and creatinine increased. Of the 7 patients with newly diagnosed AML who experienced differentiation syndrome, 6 (86%) patients recovered. Of the 34 patients with relapsed or refractory AML who experienced differentiation syndrome, 27 (79%) patients recovered after treatment or after dose interruption of TIBSOVO. Differentiation syndrome occurred as early as 1 day and up to 3 months after TIBSOVO initiation and has been observed with or without concomitant leukocytosis.

If differentiation syndrome is suspected, initiate dexamethasone 10 mg IV every 12 hours (or an equivalent dose of an alternative oral or IV corticosteroid) and hemodynamic monitoring until improvement. If concomitant noninfectious leukocytosis is observed, initiate treatment with hydroxyurea or leukapheresis, as clinically indicated. Taper corticosteroids and hydroxyurea after resolution of symptoms and administer corticosteroids for a minimum of 3 days. Symptoms of differentiation syndrome may recur with premature discontinuation of corticosteroid and/or hydroxyurea treatment. If severe signs and/or symptoms persist for more than 48 hours after initiation of corticosteroids, interrupt TIBSOVO until signs and symptoms are no longer severe.

QTc Interval Prolongation: Patients treated with TIBSOVO can develop QT (QTc) prolongation and ventricular arrhythmias. One patient developed ventricular fibrillation attributed to TIBSOVO. Concomitant use of TIBSOVO with drugs known to prolong the QTc interval (e.g., anti-arrhythmic medicines, fluoroquinolones, triazole anti-fungals, 5-HT3 receptor antagonists) and CYP3A4 inhibitors may increase the risk of QTc interval prolongation. Conduct monitoring of electrocardiograms (ECGs) and electrolytes. In patients with congenital long QTc syndrome, congestive heart failure, or electrolyte abnormalities, or in those who are taking medications known to prolong the QTc interval, more frequent monitoring may be necessary.

Interrupt TIBSOVO if QTc increases to greater than 480 msec and less than 500 msec. Interrupt and reduce TIBSOVO if QTc increases to greater than 500 msec. Permanently discontinue TIBSOVO in patients who develop QTc interval prolongation with signs or symptoms of life-threatening arrhythmia.

Guillain-Barré Syndrome: Guillain-Barré syndrome occurred in <1% (2/258) of AML patients treated with TIBSOVO in the clinical study. Monitor patients taking TIBSOVO for onset of new signs or symptoms of motor and/or sensory neuropathy such as unilateral or bilateral weakness, sensory alterations, paresthesias, or difficulty breathing. Permanently discontinue TIBSOVO in patients who are diagnosed with Guillain-Barré syndrome.

ADVERSE REACTIONS

The most common adverse reactions including laboratory abnormalities (≥20%) were hemoglobin decreased (60%), fatigue (43%), arthralgia (39%), calcium decreased (39%), sodium decreased (39%), leukocytosis (38%), diarrhea (37%), magnesium decreased (36%), edema (34%), nausea (33%), dyspnea (32%), uric acid increased (32%), potassium decreased (32%), alkaline phosphatase increased (30%), mucositis (28%), aspartate aminotransferase increased (27%), phosphatase decreased (25%), electrocardiogram QT prolonged (24%), rash (24%), creatinine increased (24%), cough (23%), decreased appetite (22%), myalgia (21%), constipation (20%), and pyrexia (20%).
In patients with newly diagnosed AML, the most frequently reported Grade ≥3 adverse reactions (≥5%) were fatigue (14%), differentiation syndrome (11%), electrocardiogram QT prolonged (11%), diarrhea (7%), nausea (7%), and leukocytosis (7%). Serious adverse reactions (≥5%) were differentiation syndrome (18%), electrocardiogram QT prolonged (7%), and fatigue (7%). There was one case of posterior reversible encephalopathy syndrome (PRES).
In patients with relapsed or refractory AML, the most frequently reported Grade ≥3 adverse reactions (≥5%) were differentiation syndrome (13%), electrocardiogram QT prolonged (10%), dyspnea (9%), leukocytosis (8%), and tumor lysis syndrome (6%). Serious adverse reactions (≥5%) were differentiation syndrome (10%), leukocytosis (10%), and electrocardiogram QT prolonged (7%). There was one case of progressive multifocal leukoencephalopathy (PML).
DRUG INTERACTIONS

Strong or Moderate CYP3A4 Inhibitors: Reduce TIBSOVO dose with strong CYP3A4 inhibitors. Monitor patients for increased risk of QTc interval prolongation.
Strong CYP3A4 Inducers: Avoid concomitant use with TIBSOVO.
Sensitive CYP3A4 Substrates: Avoid concomitant use with TIBSOVO.

QTc Prolonging Drugs: Avoid concomitant use with TIBSOVO. If co-administration is unavoidable, monitor patients for increased risk of QTc interval prolongation.

LACTATION

Because many drugs are excreted in human milk and because of the potential for adverse reactions in breastfed children, advise women not to breastfeed during treatment with TIBSOVO and for at least 1 month after the last dose.