Propanc Biopharma Analyzes Pancreatic Proenzymes Vs T-Cell Therapy Targeting Solid Tumors Such as Pancreatic, Ovarian & Colorectal Cancers

On January 11, 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 pancreatic proenzymes versus T-Cell therapy when targeting solid tumors such as pancreatic, ovarian and colorectal cancers (Press release, Propanc, JAN 11, 2021, View Source [SID1234573837]). The analysis is prepared by the Company’s Chief Executive Officer, Mr. James Nathanielsz, in collaboration with joint lead researcher, Professor Macarena Perán, from the University of Jaén, Granada, Spain.

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Cell differentiation therapy using pancreatic proenzymes has shown to degrade the fibrotic tissue on the surface of solid tumors and therefore might impair tumor engrafting, tumor niche formation and even cancer stem cell subpopulation activation. (Photo: Business Wire)
Cell differentiation therapy using pancreatic proenzymes has shown to degrade the fibrotic tissue on the surface of solid tumors and therefore might impair tumor engrafting, tumor niche formation and even cancer stem cell subpopulation activation. (Photo: Business Wire)

"We are making significant inroads in the way we treat cancer today, but there is a genuine need to continually challenge ourselves to improve the standard of care for many cancer types," said James Nathanielsz. "At Propanc, we share a vision to develop and commercialize a novel approach using pancreatic proenzymes for the long-term treatment and prevention of metastatic cancer from solid tumors. Our goal is to reduce the threat of cancer by extending life meaningfully, but not at the expense of great toxicity. This humanitarian cause affects us all."

Everybody knows what cancer is. Cells in the body begin to divide rapidly and uncontrollably in the body, with an ability to migrate from one location and spread to distant sites. However, when a cell becomes undifferentiated, forgetting how to do its job and investing all its energy in proliferating, it becomes cancerous. Unlike normal cells, cancer cells multiply, but do not differentiate. Most common therapies take advantage of the uncontrolled proliferation and kill these cells by targeting the cell division machinery. These therapies are effective, but affect healthy cells as well, particularly those with a high cell turn over, inducing undesirable effects. More recently, scientific advancements have meant that T-cell therapies are considered a tremendous improvement compared to older treatments. T-cell therapy involves using specific T-cells from the patient’s own immune system. Doctors take a type of white blood cell from the patient’s body and genetically change the cells in a lab so they can better find the cancer. Then millions of these target-seeking cells are put back into the patient.

The use of cancer-specific T-cells is a clever strategy to use the natural weapons from the body against cancer cells. This is a genuine targeted therapy, which kills cancer by recognizing antigen targets expressed on the cancer cell surface. This novel strategy is promising, although it still has some challenges. Of most importance is the health of patient’s T-cells, which may decline due to age, or degeneration induced by the cancer itself, which is not ideal. There are also limitations with regards to efficacy and safety, and they are highly expensive. Resistance can develop over time, as specific antigens mutate, causing tumor escape and disease relapse. Furthermore, a patient can have serious side effects, including very high fevers and dangerously low blood pressure days after treatment. Other serious side effects include neurotoxicity, or changes in the brain that cause swelling, confusion, seizures, or severe headaches. Another problem is that T-cells can kill off some of the good B-cells that help fight germs, so the patient may be at higher risk for infection. Finally, when factoring in all the costs associated with T-cell therapies, hospitals may charge as much as $1.5 million or more to avoid losing money.

So, whilst enhancing a patient’s immune response to attack cancer has genuine merit, other ways to stop cancer are needed to further reduce the threat of cancer from a killer disease to a chronic (long term) illness. Another approach to stop cancer is not by targeting cell death, but inducing cell differentiation. This is known as cell differentiation therapy. The key consideration is how to convince the malignant cells to stop proliferating and return to their role as a specific cell type.

So, what are the advantages of cell differentiation therapy over other strategies, like T-Cell therapy? Firstly, cell differentiation therapy does not target cell death, so healthy cells are not compromised. Cell differentiation therapy induces cancer cells to differentiate and become non-proliferative (non-replicating), so they die naturally. Cell differentiation therapy acts not only against cancer cells, but interestingly can turn cancer stem cells (undifferentiated cells) towards completely differentiated, i.e., normal cells. Significantly, once the cancer stem cells are completely differentiated, they are no longer hidden from the immune system. This means that the body’s immune response can more effectively target the cancer, and therefore, in theory, will be complementary to immunological approaches like T-Cell therapy, by improving response rates and reducing toxicity.

More than 100 years ago, a comparative embryologist Professor John Beard first proposed that pancreatic enzymes represent the body’s primary defense against cancer and would prove useful as a cancer treatment. Since then, scientists have endorsed Beard’s hypothesis with encouraging data from patient treatment. After extensive laboratory research over the last decade and limited human testing by compassionate use, there is evidence that pancreatic proenzymes reduces cancer cell growth via promotion of cell differentiation, enhances cell adhesion (cell to cell contact) and suppresses metastasis (cancer spread), has no serious side effects and improves patient survival. The unique approach targets and eradicate cancer stem cells, which can migrate to other organs triggering explosive tumor growth, causing the patient to relapse after standard treatments that do not target non-dividing cells. Eighty percent of cancers are from solid tumors and metastasis is the main cause of patient death, therefore the potential of cell differentiation therapy using pancreatic proenzymes is significant. Given they are derived from natural sources, pancreatic proenzymes are also not cost prohibitive.

There is little doubt that both the T-Cell based and cell differentiation therapy approaches have emerged to address the limited efficacy of chemotherapy and radiation therapy for patients with advanced solid tumors. Although both therapies bear a slight resemblance because they enhance the immune response, they are not comparable by their mode of action. It is also understood the tumor micro-environment promotes the appearance of new cancer stem cells, derived from non-stem cancerous cells by secreting several biomarkers, such as IL6 (interleukin 6), HGF (hepatocyte growth factor), or TGFβ-163 (tumor growth factor beta-163). Consequently, it is critical to impact the tumor micro-environment in order to effectively eradicate the tumor. Cell differentiation therapy using pancreatic proenzymes has shown to degrade the fibrotic tissue on the surface of solid tumors and therefore might impair tumor engrafting, tumor niche formation and even cancer stem cell subpopulation activation.

Whilst T-Cell therapy has helped to advance the treatment of cancer, there are new and exciting approaches which are complementary and may provide a long-term solution to the treatment and prevention of metastatic cancer from most common solid tumors. Cell differentiation therapy using pancreatic proenzymes is based on the original work by John Beard, a professor of embryology at Edinburgh University over 100 years ago, using fresh pancreatic extracts. Through advancements in science and technology, there is an opportunity to introduce an improved version of this hypothesis, as a long-term therapeutic approach to treat metastatic cancer from solid tumors, which today, remains the main cause of patient death for sufferers.

Bibliography

"Antitumor efficacy of chymotrypsinogen and trypsinogen," P. Hernández, E. López-Ruiz, M. A. García, J. A. Marchal, J. Kenyon, M. Perán.
"In vitro treatment of carcinoma cell lines with pancreatic (pro)enzymes suppresses the EMT programme and promotes cell differentiation", M. Perán, J.A. Marchal, M.A. García, J. Kenyon & D. Tosh.
"A formulation of pancreatic proenzymes provides potent anti-tumour efficacy: a pilot study focused on pancreatic and ovarian cancer", M. Perán, E. López-Ruiz, M. A. García, S. Nadaraia-Hoke, R. Brandt, J. A. Marchal & J. Kenyon.
"Pancreatic proenzymes treatment suppresses BXPC-3 pancreatic Cancer Stem Cell subpopulation and impairs tumour engrafting," P. Hernández-Camarero, E. López-Ruiz, C. Griñán-Lisón, M.A. García, C. Chocarro-Wrona, J.A. Marchal, J. Kenyon & M. Perán.
"Trypsinogen and Chymotrypsinogen: Potent Anti-Tumour Agents," A. González-Titos, P. Hernández-Camarero, S. Barungi, J.A. Marchal, J. Kenyon & M. Perán. *
*Draft manuscript under review

Arcus Biosciences to Present Preliminary Data from Phase 1 Portion of ARC-8 Study for AB680 in Metastatic Pancreatic Cancer at ASCO-GI Symposium

On January 11, 2021 Arcus Biosciences, Inc. (NYSE:RCUS), an oncology-focused biopharmaceutical company working to create best-in-class cancer therapies, reported that preliminary data from the ongoing dose-escalation portion of its ARC-8 Phase 1/1b study, evaluating the safety and tolerability of AB680, the first small-molecule CD73 inhibitor to enter the clinic, in combination with zimberelimab (anti-PD-1) and nab-paclitaxel plus gemcitabine (chemotherapy) in front-line metastatic pancreatic cancer will be presented in a poster session at the ASCO (Free ASCO Whitepaper) 2021 Virtual Gastrointestinal Cancers Symposium (ASCO GI) being held January 15th – 17th, 2021 (Press release, Arcus Biosciences, JAN 11, 2021, View Source [SID1234573853]).

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"While recent cancer breakthrough therapies, most notably anti-PD-1 antibodies, have led to dramatic improvements in outcomes in many cancer settings, this is not the case for pancreatic cancer, which remains a devastating diagnosis for patients. We are highly encouraged by the preliminary data from our Phase 1 trial for AB680 in combination with anti-PD-1 therapy and chemotherapy, in which we have seen promising clinical activity in these difficult to treat patients. Importantly, this experimental regimen has been well tolerated, and early safety data indicate that this AB680 combination regimen appears to have a side effect profile similar to that of anti-PD-1 therapy and chemotherapy," said Bill Grossman, M.D., the Chief Medical Officer of Arcus. "We look forward to presenting updated data from the Phase 1 portion of this trial at ASCO (Free ASCO Whitepaper) GI on January 15th, wherein we will report more mature safety and clinical response data, including those from the 100mg dose cohort."

The clinical activity and safety profile observed to date with AB680 in combination with zimberelimab (anti-PD-1 antibody) and chemotherapy support its recent advancement into the ongoing Phase 1b expansion portion of the study, as well as plans to open a randomized control arm for the Phase 1b expansion. Dosing of AB680 100mg I.V. every two weeks has been selected for this portion of the study.

Full details of the presentation are as follows:

Abstract/Poster Title: ARC-8: Phase I/Ib study to evaluate safety and tolerability of AB680 + chemotherapy + zimberelimab (AB122) in patients with treatment-naive metastatic pancreatic adenocarcinoma (mPDAC)
Abstract No: 404
Poster Session: Pancreatic Cancer
Available Date: January 15, 2021
Time: 5:00 a.m. PT

In addition to the presentation on AB680, Arcus will also highlight the design of the recently initiated ARC-9 randomized Phase 2 study to advance etrumadenant in late-line colorectal cancer:

Abstract/Poster Title: ARC-9: Phase Ib/II study to evaluate etrumadenant (AB928)-based treatment combinations in patients with metastatic colorectal cancer (mCRC)
Abstract No: TPS150
Trials in Progress Poster Session: Colorectal Cancer
Available Date: January 15, 2021
Time: 5:00 a.m. PT

Pancreatic Cancer

Pancreatic cancer is the fourth leading cause of cancer-related deaths in Europe and the United States1 and the seventh leading cause of cancer-related deaths worldwide2.

Pancreatic ductal adenocarcinoma (PDAC) is the most prevalent neoplastic disease of the pancreas, with high metastatic potential, accounting for more than 90% of all pancreatic malignancies and is a highly devastating disease with poor prognosis and rising incidence.3,4

Few treatment options exist for metastatic pancreatic cancer, and response rates to the standard of care therapy of gemcitabine/nab-paclitaxel remain very low. Based on the FDA approved label for nab-paclitaxel in combination with gemcitabine, the phase 3 registrational trial demonstrated overall and complete response rates in patients with metastatic pancreatic cancer that were 23% and <1%, respectively. 1,5

To date, addition of anti-PD-1 antibodies to gemcitabine/nab-paclitaxel in controlled clinical trials in this setting has shown no added benefit when compared to that obtained with the chemotherapy alone.6,7

About ARC-8 Study

ARC-8 is a Phase 1/1b study to evaluate safety and tolerability of AB680 + zimberelimab (AB122) + chemotherapy in patients with treatment-naive metastatic pancreatic adenocarcinoma.

For additional information on this trial (NCT04104672), please visit www.clinicaltrials.gov.

About AB680

AB680 is an extremely potent and selective small-molecule CD73 inhibitor designed to provide differential benefits relative to monoclonal antibodies, such as greater inhibition of CD73 enzymatic activity (both soluble and cell-bound) and deeper tumor penetration. CD73 is the primary enzymatic producer of immunosuppressive adenosine in the tumor microenvironment, and high CD73 expression is associated with significantly poorer prognosis in several tumor types, including pancreatic cancer. 8 By effectively eliminating CD73-derived adenosine, AB680 may improve the efficacy of treatment approaches expected to elicit anti-cancer immune responses (e.g., platinum-based chemotherapy with/without anti-PD-1 therapy). AB680 was the first small-molecule CD73 inhibitor to enter the clinic and demonstrated a favorable safety profile with a long half-life in a healthy volunteer study. AB680 is currently in a Phase 1/1b study for the treatment of first-line metastatic pancreatic cancer.

TURNING POINT AND ZAI LAB BROADEN COLLABORATION

On January 11, 2021 Turning Point Therapeutics, Inc. (NASDAQ: TPTX), a precision oncology company developing next-generation therapies that target genetic drivers of cancer, and Zai Lab (NASDAQ: ZLAB; HKEX: 9688), an innovative commercial-stage biopharmaceutical company, reported an expansion of their collaboration (Press release, Zai Laboratory, JAN 11, 2021, View Source [SID1234573787]).

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Under the terms of the new agreement, Zai Lab will obtain exclusive rights to develop and commercialize TPX-0022, Turning Point’s MET, SRC and CSF1R inhibitor, in Greater China, which includes mainland China, Hong Kong, Macau and Taiwan. Turning Point will receive a $25 million upfront payment, with up to approximately $336 million in potential development, regulatory and sales-based milestone payments. Turning Point will also be eligible to receive mid-teen- to low-twenty-percent royalties based on annual net sales of TPX-0022 in Greater China. In addition, Turning Point will have the right of first negotiation to develop and commercialize an oncology drug candidate discovered by Zai Lab.

This agreement builds on Zai Lab and Turning Point’s existing relationship under the exclusive licensing agreement announced by the companies in July 2020, under which Zai Lab gained the exclusive right to develop and commercialize Turning Point’s lead drug candidate, repotrectinib, in Greater China.

"The higher incidence of MET-driven cancers – particularly in gastric and lung cancer – in Asian countries led us to initiate the development of TPX-0022 in Greater China following our encouraging initial data from the Phase 1 SHIELD-1 study," said Athena Countouriotis, M.D., president and chief executive officer of Turning Point. "We have great confidence in Zai Lab as our partner to advance this important drug candidate in a key region of the world. Zai Lab also has a promising discovery pipeline and we are pleased to receive the right of first negotiation for a drug candidate from Zai’s discovery pipeline."

Dr. Samantha Du, Founder, Chairperson and Chief Executive Officer of Zai Lab, said, "Turning Point has assembled a formidable pipeline of next-generation oncology target therapies, and we are very pleased to broaden our global collaboration and strategic partnership. We believe TPX-0022 is a promising drug candidate that is also highly synergistic with our portfolio in gastric and lung cancer."

Jin Li, M.D., Professor, Chairman of Chinese Society of Clinical Oncology Foundation and Director of Department of Oncology, Tongji University Shanghai East Hospital said, "The initial safety and efficacy data for TPX-0022 are promising, and its novel mechanism to target MET, SRC and CSF1R encourages us to investigate its therapeutic potential further. We are particularly interested in the early but promising findings in patients with MET-driven gastric cancer and look forward to advancing the study of TPX-0022 in this area of high unmet need in China."

Initial data from the SHIELD-1 study reported in a late-breaker oral presentation at the EORTC-NCI-AACR (Free EORTC-NCI-AACR Whitepaper) symposium highlighted preliminary clinical activity, including objective responses across multiple tumor types and a generally tolerable safety profile.

About TPX-0022

TPX-0022 is an orally bioavailable multi-targeted kinase inhibitor with a novel three-dimensional macrocyclic structure that inhibits the MET, CSF1R (colony stimulating factor 1 receptor) and SRC kinases. TPX-0022 has completed IND-enabling studies and cleared its IND. During the second half of 2019, Turning Point initiated the SHIELD-1 Phase 1 clinical trial of TPX-0022 for the treatment of advanced or metastatic solid tumors with abnormal MET/HGF or CSF1R/SCF1R signaling.

MET is a receptor tyrosine kinase that binds with high affinity to hepatocyte growth factor (HGF). MET alterations, including point mutations, amplifications, fusions, exon 14 skipping, and the generation of HGF-MET autocrine loops have been reported in many cancers. MET amplification has been detected in up to 20 percent of non-small cell lung cancer patients with EGFR mutations who acquired resistance to Iressa (gefitinib), Tarceva (erlotinib) or Tagrisso (osimertinib) treatment. SRC is a kinase involved in the MET signaling pathway. Inhibition of SRC has the potential to reduce or abolish the upregulation of HGF. Targeting CSF1R leads to the modulation of tumor-associated macrophages (TAMs), a type of immune cell that suppresses the T-cell mediated anti-tumor immune response, which is a promising therapeutic strategy for TPX-0022 as a single agent or in combination with standard of care chemotherapy and immunotherapy in various solid tumors.

MacroGenics to Participate in Upcoming Investor Conferences

On January 11, 2021 MacroGenics, Inc. (Nasdaq: MGNX), a biopharmaceutical company focused on developing and commercializing innovative monoclonal antibody-based therapeutics for the treatment of cancer, reported that the Company’s management will participate in the following investor conferences in January (Press release, MacroGenics, JAN 11, 2021, View Source [SID1234573805]):

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H.C. Wainwright & Co. BioConnect 2021 Conference. A corporate overview provided by MacroGenics’ management will be available for on-demand viewing from January 11 – 14, 2021. In addition, MacroGenics’ President & Chief Executive Officer, Scott Koenig, M.D., Ph.D., will participate in a panel discussion on Precision Medicine hosted by Scott Gottlieb, M.D., Former Commissioner of the U.S. Food and Drug Administration. The panel will cover the importance of biomarkers and cytogenetic profiling in drug discovery, development and commercialization and will take place on Wednesday, January 13, 2021, at noon ET.
39th Annual J.P. Morgan Healthcare Conference. MacroGenics’ management will participate in one-on-one meetings and provide a corporate overview on January 14, 2021 at 10:00 AM ET.
Webcasts of the above presentations may be accessed under "Events & Presentations" in the Investor Relations section of MacroGenics’ website at View Source The Company will maintain archived replays of these webcasts on its website for 30 days after each conference.

Aileron Therapeutics Announces Completion of $35.9 Million Registered Direct Offering with Participation by New Fundamental Healthcare Investors Acorn Bioventures, BVF Partners, L.P. and Maven Investment Partners

On January 11, 2021 Aileron Therapeutics, Inc. (Nasdaq: ALRN) reported the completion of its previously announced registered direct offering of 32,630,983 of its shares of common stock at a purchase price of $1.10 per share, for gross proceeds of $35.9 million, before deducting placement agent fees and other offering expenses payable by Aileron (Press release, Aileron Therapeutics, JAN 11, 2021, View Source [SID1234573822]). Aileron is developing ALRN-6924 as a novel medicine to selectively protect healthy cells in patients with cancers that harbor p53 mutations to reduce or eliminate chemotherapy-induced side effects while preserving chemotherapy’s effects against cancer cells, a concept known as chemoprotection.

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New fundamental investors, including Acorn Bioventures, BVF Partners, L.P., Maven Investment Partners and Grand Oaks Capital, participated in the offering, in addition to several existing Aileron investors, including Satter Medical Technology Partners and Lincoln Park Capital Fund, LLC.

JonesTrading Institutional Services LLC ("JonesTrading") acted as the placement agent for the offering.

In addition to the $35.9 million registered direct offering, between November 12, 2020 and January 5, 2021, Aileron sold an aggregate of 9,894,519 shares of its common stock in "at the market" offerings under the Capital on DemandTM Sales Agreement with JonesTrading resulting in aggregate gross proceeds of approximately $12.7 million. Gross proceeds combined from both offerings were $48.6 million before deducting commissions and fees.

With the proceeds from these transactions, Aileron believes that its cash, cash equivalents and investments will enable it to fund its current strategic plan into the second half of 2023, including the planned clinical trial of ALRN-6924 in patients with advanced non-small cell lung cancer (NSCLC).

"We are thrilled to welcome Acorn Bioventures, BVF Partners and Maven Investment Partners as fundamental healthcare investors in Aileron. We believe that the participation of these funds, in addition to the continued support of key existing Aileron investors, is further validation of the potential of ALRN-6924 as an important medicine in the emerging chemoprotection field," said Manuel Aivado, M.D., Ph.D., President and Chief Executive Officer of Aileron. "With the completed offering, we are well positioned to continue advancing toward our vision to bring chemoprotection to all patients with p53-mutant cancer regardless of cancer type or chemotherapy."

Dr. Aivado continued, "For decades, the medical community has largely been resigned to the sad reality that chemotherapy destroys healthy cells while destroying cancer cells. 2021 holds the promise to begin a shift in this long-held mindset with the imminent PDUFA date and potential approval of the industry’s first chemoprotective agent1 that, similar to ALRN-6924, aims to protect healthy cells from chemotherapy’s side effects. Given the increasing interest in chemoprotection and the significant unmet medical need, we believe ALRN-6924 has the potential to have an important and broad role in proactively preventing chemotherapy’s harmful effects on cancer patients."

Aileron plans to begin enrollment in a Phase 1b randomized, double-blind, placebo-controlled clinical trial of ALRN-6924 in patients with advanced p53-mutated NSCLC undergoing treatment with first-line carboplatin doublet chemotherapy (with or without immune checkpoint inhibitors), in the second quarter of 2021. The planned Phase 1b NSCLC trial follows Aileron’s presentation in October 2020 of clinical data from its ongoing Phase 1b clinical trial of ALRN-6924 in small cell lung cancer (SCLC) demonstrating clinical proof-of-concept that treatment with ALRN-6924 resulted in a protective effect against severe anemia, thrombocytopenia and neutropenia in patients with p53-mutated SCLC treated with topotecan. Aileron anticipates reporting initial results from the trial late in the fourth quarter of 2021 and full results in mid-2022.

This press release shall not constitute an offer to sell or the solicitation of an offer to buy these securities, nor shall there be any sale of these securities in any state or other jurisdiction in which such offer, solicitation or sale would be unlawful prior to the registration or qualification under the securities laws of any such state or other jurisdiction.

How ALRN-6924 Is Designed to Protect Healthy Cells from Chemotherapy

ALRN-6924 is being developed by Aileron as a novel chemoprotective medicine to selectively protect healthy cells in patients with cancers that harbor p53 mutations to reduce or eliminate chemotherapy-induced side effects.

Chemotherapy preferentially acts on cells that are cycling or undergoing the process of cell division. In cancer cells, the cell cycle is unchecked, which leads to uncontrolled cell proliferation, a hallmark of cancer. Certain types of healthy cells also naturally need to cycle, such as bone marrow cells, hair follicle cells, skin cells, and cells lining the oral cavity and the gastrointestinal tract. As a result, chemotherapy preferentially targets and kills both cycling healthy cells and cycling cancer cells. This, in turn, can lead to a spectrum of chemotherapy-induced side effects, from unpleasant to life-threatening and fatal.

ALRN-6924, an investigational first-in-class MDM2/MDMX dual inhibitor, is administered prior to chemotherapy to patients with p53-mutant cancers. ALRN-6924 is designed to activate normal p53 protein in patients’ healthy cells, temporarily and reversibly pausing cell cycling to selectively shield the patients’ healthy cells from chemotherapy. The protection is limited to healthy cells, as ALRN-6924 cannot work in p53-mutated cancer cells given that mutated p53 has lost its function in those cells. Therefore, cancer cells continue to cycle uninterrupted and remain fully susceptible to destruction by chemotherapy.

1 The U.S. Food & Drug Administration has assigned a Prescription Drug User Fee Act (PDUFA) date of February 15, 2021 for G1 Therapeutics, Inc.’s investigational therapy trilaciclib.