A Multiregional, Randomized, Double-Blinded, Placebo-Controlled Phase 3 Study of Lerociclib With Letrozole, Versus Placebo in Combination With Letrozole, in Participants With Advanced/Metastatic or Recurrent, Grade 1 or Grade 2 Endometrioid Endometrial Carcinoma

This is a randomized, double-blinded, placebo-controlled Phase 3 clinical trial to compare the combination of lerociclib (administered at 150 mg twice a day (BID) with letrozole (administered at 2.5 mg once a day (QD) to that of placebo with letrozole (2.5 mg QD) in female participants with Grade 1 or Grade 2 (ie, low-grade histology) endometrioid endometrial cancer (EC) and advanced/metastatic or recurrent disease.
The study population will consist of female participants with endometrioid EC who are treatment-naïve in the advanced/metastatic setting (ie, the first-line [1L] population). Participants may have received prior adjuvant chemotherapy/chemoradiation for localized disease if the adjuvant therapy was administered ≥ 6 months prior. All participants must also be naïve to prior endocrine therapy for EC, and confirmed as medically postmenopausal to be eligible.
The study will comprise a Screening Period of up to 28 days in duration; a Study Treatment Phase; a Safety Follow-up Period spanning the time of study treatment discontinuation-including discontinuation due to confirmed disease progression, as applicable-through 28 days after the participant's last dose of any study intervention or the start of subsequent anticancer therapy (whichever occurs first); and a Survival Follow-up Period that will continue until the participant's death or until at least 50% of all study participants have died (whichever occurs first).
While receiving their randomized assigned study treatment, participants will undergo imaging assessments via computed tomography (CT) of the chest/abdomen/pelvis with contrast- or, if CT is medically contraindicated (eg, due to iodine allergy), via magnetic resonance imaging (MRI) with gadolinium-every 8 weeks for the first 12 months and then every 12 weeks thereafter.

Start Date18 Apr 2023

Sponsor / Collaborator

EQRx International, Inc.

[+2]

NCT05860582 / CompletedPhase 1

A Study of [14C]GB491 on Mass Balance and Biotransformation in Chinese Male Healthy Subjects

This is an open-label, single-center study to evaluate the mass-balance and pharmacokinetics of GB491 in 4-8 healthy male subjects receiving a single oral 150mg dose of GB491 containing approximately 50 uCi of [14C]GB491. This study will help understand how the drug appears in the blood, urine, and feces after it is administered.
In addition, this study will also evaluate the safety of a single dose of [14C]GB491 when given to healthy subjects.

Start Date14 Sep 2022

Sponsor / Collaborator

Genor Biopharma Co., Ltd.

NCT05851014 / RecruitingPhase 3

A Randomized, Double-Blind, Placebo-Controlled Phase III Trial of GB491 in Combination With Letrozole in Subjects With HR Positive and HER2 Negative Locally Advanced or Metastatic Breast Cancer Who Have Not Previously Received Systemic Therapy in This Disease Setting

The main purpose of this study is to evaluate the efficacy and safety of GB491 combined with Letrozole versus placebo combined with Letrozole in the treatment of HR+/HER2- locally advanced or metastatic breast cancer without prior systemic antitumor therapy

Start Date14 Jan 2022

Sponsor / Collaborator

Genor Biopharma Co., Ltd.

100 Clinical Results associated with Lerociclib

100 Translational Medicine associated with Lerociclib

100 Patents (Medical) associated with Lerociclib

Literatures (Medical) associated with Lerociclib

01 Mar 2024·Journal of Pediatric Surgery

CDK4/6 Inhibition With Lerociclib is a Potential Therapeutic Strategy for the Treatment of Pediatric Sarcomas

Article

Author: Yoon, Karina J ; Stewart, Jerry E ; Beierle, Andee M ; Beierle, Elizabeth A ; Horton, Sara C ; Aye, Jamie ; Julson, Janet R ; Bownes, Laura V ; Quinn, Colin H

BACKGROUNDSarcomas are a heterogenous collection of bone and soft tissue tumors. The heterogeneity of these tumors makes it difficult to standardize treatment. CDK 4/6 inhibitors are a family of targeted agents which limit cell cycle progression and have been shown to be upregulated in sarcomas. In the current preclinical study, we evaluated the effects of lerociclib, a CDK4/6 inhibitor, on pediatric sarcomas in vitro and in 3D bioprinted tumors.METHODSThe effects of lerociclib on viability, proliferation, cell cycle, motility, and stemness were assessed in established sarcoma cell lines, U-2 OS and MG-63, as well as sarcoma patient-derived xenografts (PDXs). 3D printed biotumors of each of the U-2 OS, MG-63, and COA79 cells were utilized to study the effects of lerociclib on tumor growth ex vivo.RESULTSCDK 4/6, as well as the intermediaries retinoblastoma protein (Rb) and phosphorylated Rb were identified as targets in the four sarcoma cell lines. Lerociclib treatment induced cell cycle arrest, decreased proliferation, motility, and stemness of sarcoma cells. Treatment with lerociclib decreased sarcoma cell viability in both traditional 2D culture as well as 3D bioprinted microtumors.CONCLUSIONSInhibition of CDK 4/6 activity with lerociclib was efficacious in traditional 2D sarcoma cell culture as well as in 3D bioprints. Lerociclib holds promise and warrants further investigation as a novel therapeutic strategy for management of these heterogenous groups of tumors.

01 Apr 2020·Breast Cancer Research and TreatmentQ2 · MEDICINE

G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer

Q2 · MEDICINE

Article

Author: Baldi, Robert ; Xiong, Rui ; Baker, Jennifer G ; Heetderks, Kendall A ; Wardell, Suzanne E ; Chao, Christina A ; Bae, Yeeun ; Norris, John D ; Zhao, Jiong ; Strum, Jay C ; Tonetti, Debra A ; Desautels, Taylor K ; Thatcher, Gregory R J ; Thompson, Delita A ; Gutgesell, Lauren M ; Sorrentino, Jessica A ; Andreano, Kaitlyn J ; Bisi, John E

AbstractPurposeThe combination of targeting the CDK4/6 and estrogen receptor (ER) signaling pathways with palbociclib and fulvestrant is a proven therapeutic strategy for the treatment of ER-positive breast cancer. However, the poor physicochemical properties of fulvestrant require monthly intramuscular injections to patients, which limit the pharmacokinetic and pharmacodynamic activity of the compound. Therefore, an orally available compound that more rapidly reaches steady state may lead to a better clinical response in patients. Here, we report the identification of G1T48, a novel orally bioavailable, non-steroidal small molecule antagonist of ER.MethodsThe pharmacological effects and the antineoplastic mechanism of action of G1T48 on tumors was evaluated using human breast cancer cells (in vitro) and xenograft efficacy models (in vivo).ResultsG1T48 is a potent and efficacious inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells, similar to the pure antiestrogen fulvestrant. In addition, G1T48 can effectively suppress ER activity in multiple models of endocrine therapy resistance including those harboring ER mutations and growth factor activation. In vivo, G1T48 has robust antitumor activity in a model of estrogen-dependent breast cancer (MCF7) and significantly inhibited the growth of tamoxifen-resistant (TamR), long-term estrogen-deprived (LTED) and patient-derived xenograft tumors with an increased response being observed with the combination of G1T48 and the CDK4/6 inhibitor lerociclib.ConclusionsThese data show that G1T48 has the potential to be an efficacious oral antineoplastic agent in ER-positive breast cancer.

27 Jun 2017·Oncotarget

Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors

Article

Author: Sorrentino, Jessica A. ; Bisi, John E. ; Darr, David D. ; Strum, Jay C. ; Roberts, Patrick J. ; Jordan, Jamie L. ; Tavares, Francis X.

Inhibition of the p16INK4a/cyclin D/CDK4/6/RB pathway is an effective therapeutic strategy for the treatment of estrogen receptor positive (ER+) breast cancer. Although efficacious, current treatment regimens require a dosing holiday due to severe neutropenia potentially leading to an increased risk of infections, as well as tumor regrowth and emergence of drug resistance. Therefore, a next generation CDK4/6 inhibitor that can inhibit proliferation of CDK4/6-dependent tumors while minimizing neutropenia could reduce both the need for treatment holidays and the risk of inducing drug resistance.Here, we describe the preclinical characterization and development of G1T38; a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor. In vitro, G1T38 decreased RB1 (RB) phosphorylation, caused a precise G1 arrest, and inhibited cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines including breast, melanoma, leukemia, and lymphoma cells. In vivo, G1T38 treatment led to equivalent or improved tumor efficacy compared to the first-in-class CDK4/6 inhibitor, palbociclib, in an ER+ breast cancer xenograft model. Furthermore, G1T38 accumulated in mouse xenograft tumors but not plasma, resulting in less inhibition of mouse myeloid progenitors than after palbociclib treatment. In larger mammals, this difference in pharmacokinetics allowed for 28 day continuous dosing of G1T38 in beagle dogs without producing severe neutropenia. These data demonstrate G1T38 has unique pharmacokinetic and pharmacodynamic properties, which result in high efficacy against CDK4/6 dependent tumors while minimizing the undesirable on-target bone marrow activity, thus potentially allowing G1T38 to be used as a continuous, daily oral antineoplastic agent.

News (Medical) associated with Lerociclib

30 Oct 2024

·www.biospace.com

10 Years of NextGen Honorees: Where Are They Now?

iStock, leolintang BioSpace has been compiling a list of the most innovative and exciting biotechs for a decade. Here we take a look back at noteworthy companies from each of those lists. 2024 marked the 10th year of BioSpace ’s NextGen list, a collection of biotechs that are on the cutting edge and poised to break barriers in the industry. As we prep next year’s list, to be released in January, we decided to take a look back at a notable honoree from each of our past lists. There were many fascinating companies that have gone on to great things; on the other hand, sometimes things don’t go as well as we predicted. We have a few not-so-great stories to tell, too. ___________________________________________ 2024 ReNAgade Therapeutics Status: Bought by Orna Therapeutics This company made our list for a pretty big reason: a massive $300 million series A in one of the toughest financing environments in recent memory. The company was launched in May 2023 to develop RNA medicines to treat diseases anywhere in the body. One of the lead investors in the round was MPM BioImpact, whose managing partner Ansbert Gadicke founded ReNAgade. Early in the biotech’s history as a stealth company, there was a bit of foreshadowing as to where the company would end up. ReNAgade struck up a partnership with Orna Therapeutics, which was also working on RNA therapeutics. The work attracted the attention of Merck in a deal worth up to $3.5 billion with development and commercialization milestones. Given the money on the line, Orna went all in on ReNAgade, buying out the biotech in May of this year—almost a year to the day after its launch. Financial details were not disclosed. See the full class of 2024 . ___________________________________________ 2023 Mariana Oncology Status: Bought by Novartis What a year 2023 turned out to be for Mariana Oncology. After raising a $175 million series B in September of that year, the company was bought out by Novartis for $1 billion , plus $750 million in milestones. Originally known as Curie Therapeutics, Mariana emerged from stealth with a $75 series A raise in December 2021 to develop new radiopharmaceuticals. The company caught our eye and made the 2023 list, but apparently Novartis was keeping an eye too. The radiopharmaceutical-hungry Big Pharma said at the time of the deal that Mariana’s technology would help it double down in the field of radioligand therapeutics. On a recent earnings call, Novartis executives expressed their excitement in the Mariana technology, saying that candidates from the buyout are speeding toward the clinic and could go after well-established antibody-drug conjugate (ADC) targets. See the full class of 2023 . ___________________________________________ 2022 Eikon Therapeutics Status: Operating Eikon has spent the two years since landing on our list racking up cash and poaching executives from CEO Rodger Perlmutter’s former employer Merck. The biotech’s raises have been huge in a really tough market: a $148 million series A in May 2021, $518 million for a January 2022 series B and most recently, $106 million in series C financing in June 2023 . At the most recent raise, Eikon also announced the acquisition of a clinical pipeline. The company now boasts oncology assets in Phase I and II testing for non-small cell lung cancer and melanoma, respectively. The rest of Eikon’s pipeline is in preclinical research or discovery. See the full class of 2022 . ___________________________________________ 2021 EQRx Status: Bought by Revolution Medicines, assets terminated EQRx emerged with a lofty goal we could all get behind: develop drugs at a lower cost. It raised a cool $200 million in a July 2020 series A, then caught the special purpose acquisition company (SPAC) wave to the Nasdaq just over a year later, adding $1.8 billion in an August 2021 IPO. The company was helmed at first by serial biotech entrepreneur Alexis Borisy. Trouble emerged shortly thereafter, with EQRx cutting lead asset sugemalimab for NSCLC after determining it had no path to market. The company shifted to two other assets, aumolertinib and lerociclib, but later dropped the former. Several rounds of layoffs made the company ever smaller before EQRx finally gave up entirely. The assets were terminated as Revolution Medicines bought out the company and its hefty $1 billion bank account. Borisy has since gone on to start a venture capital firm called Curie.Bio . See the full class of 2021 . ___________________________________________ 2020 Cerevel Therapeutics Status: Bought by AbbVie Cerevel as a company is no more, but its medicines live on at AbbVie, which bought the biotech for $8.7 billion in December 2023. The deal was part of a trend of neuroscience-focused biotechs being bought up by Big Pharma, with Cerevel moving in the same month as Bristol Myers Squibb bought Karuna Therapeutics for $14 billion. BMS was rewarded quickly with a recent FDA approval for KarXT (now Cobenfy) for schizophrenia, but AbbVie too has had success since sealing the deal. Cerevel’s investigational Parkinson’s disease therapy tavapadon improved control of motor symptoms when used with common treatment levodopa in a Phase III trial that read out in April. The data would support a regulatory filing for the therapy, executives said at the time. Two additional late-stage readouts for the therapy are due later this year. But the real star of the deal was emraclidine, which is in Phase III studies for schizophrenia. Cerevel also brought a major depression treatment to the table. “These assets clearly will be great additions to our neuroscience franchise,” said AbbVie’s CEO Rob Michael on the company’s second quarter earnings call. See the full class of 2020 . ___________________________________________ 2019 Genevant Status: Operating One of Roivant’s offshoots, Genevant is still operating today, working on developing nucleic acid delivery technology. Just last week, Genevant signed a deal with CRISPR gene editing company Editas Medicines to develop in vivo gene editing medicines for two undisclosed targets. Genevant has also recently signed deals with Novo Nordisk, Tome Biosciences, Gritstone bio and Repair Biotechnologies. But perhaps the most compelling story from Genevant since we named them to our NextGen list has been their litigation with famed biotech Moderna over the lipid nanoparticle delivery system used for its approved COVID-19 vaccine. Genevant and Arbutus Biopharma filed several patent infringement claims against Moderna arguing that the vaccine developer used their technology without license or proper compensation. A judge sided with Arbutus and Genevant in April, with a trial set for next year. See the full class of 2019 . ___________________________________________ 2018 BlueRock Therapeutics Status: Bought by Bayer Bayer bought cell therapy biotech BlueRock Therapeutics in August 2019 for $1 billion, but rather than absorbing the company into itself, the German pharma kept the name and unit operating. This unusual but refreshing strategy means that the company essentially lives on. In June 2023, BlueRock reported that Parkinson’s disease stem cell therapy bemdaneprocel was well tolerated with no significant side effects in a Phase I trial with 12 patients. It was the first cell therapy to show positive results in human testing, Bayer said at the time. A September update showed similar safety results. The therapy has since received a regenerative medicine advanced therapy tag from the FDA. Elsewhere in the pipeline, BlueRock’s investigational iPSC-derived cell therapy OpCT-001 for certain retinal disorders was cleared for human testing in September. The therapy was licensed from FUJIFILM Cellular Dynamics and Opsis Therapeutics. See the full class of 2018 . ___________________________________________ 2017 Decibel Therapeutics Status: Bought by Regeneron Regeneron made a splash at this year’s American Society of Gene and Cell Therapy meeting in Baltimore when it showcased results of a Phase I/II trial of hearing loss therapy DB-OTO. The therapy restored hearing in two children who had a genetic form of hearing loss. While Regeneron’s branding was behind the conference presentation, the gene therapy came from Decibel Therapeutics. Regeneron bought the biotech for $109 million in August 2023, at which point the two companies had already been working together for six years. The biotech was integrated into Regeneron’s genetic medicines portfolio. See the full class of 2017 . ___________________________________________ 2016 CRISPR Therapeutics Status: Operating CRISPR Therapeutics made history last year as the first company, along with partner Vertex Pharmaceuticals, to gain an FDA approval for a CRISPR-based gene edited therapy. The companies were granted an FDA greenlight for Casgevy in sickle cell disease. The same day, bluebird bio got a similar nod for a competing gene therapy, though not one that involves CRISPR technology. The FDA approval was a triumph of modern biotechnology. But the roll out has been slow given the nature of gene therapy treatment, and only recently have patients begun receiving infusions of the medicine. Casgevy is now also approved for beta thalassemia, another blood disorder. The company has turned to the rest of its pipeline, including a CD19-directed CAR T cell program called CTX112, which is being tested in both cancer and autoimmune disorders. CTX131 is in development for hematological malignancies as well. CEO Sam Kulkarni has expressed confidence in CRISPR’s leading position in gene editing and pledged to be on top of emerging technologies. “One of the most important considerations for us is that we don’t get disrupted,” he said at the Goldman Sachs healthcare conference in June. “We are the leaders in the gene editing space and we have been, but we want to make sure that we’re looking at every improvement that’s coming out there.” See the full class of 2016 . ___________________________________________ 2015 Spark Therapeutics Status: Bought by Roche Like BlueRock, Spark Therapeutics was folded into a Big Pharma but kept its identity. Spark earned a spot on our very first NextGen list in 2015 thanks to its active clinical hemophilia program and fundraises totaling $122.8 million. The company caught the eye of Roche, which swooped in with a $4.8 billion bid in February 2019. The deal eventually turned into a bit of a boondoggle, with regulatory delays slowing things down until it finally closed that December. At issue was Roche’s hemophilia Hemlibra. Regulators worried that Spark’s hemophilia program and Hemlibra together could stifle competition and create a monopoly. Spark brought with it the approved eye disease gene therapy Luxturna. With the deal closed, Spark has charged forward under the Roche banner. The unit is developing a 500,000-square foot Gene Therapy Innovation Center in Philadelphia as its flagship manufacturing space. See the full class of 2015 .

Phase 1AcquisitionPhase 3Drug Approval

22 May 2024

·www.biospace.com

G1 Therapeutics and Deimos Biosciences Announce Global (Excluding Asia-Pacific) License Agreement for Lerociclib for Radioprotective Uses

Jupiter Bioventures will Gain Exclusive Rights for the Clinical Development, Regulatory Submissions, and Commercialization of Lerociclib for Radioprotection in the US, Europe, Japan, and All Other Global Markets Excluding Asia-Pacific RESEARCH TRIANGLE PARK, N.C. and SAN FRANCISCO, May 22, 2024 (GLOBE NEWSWIRE) -- G1 Therapeutics, Inc. (Nasdaq: GTHX), a commercial-stage oncology company, and Deimos Biosciences, a portfolio company of Jupiter Bioventures, announced a global licensing agreement (excluding the Asia-Pacific region) for lerociclib for radioprotective uses. Lerociclib is a potent and selective inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6). Such inhibitors can increase the survival of animals exposed to radiation. Jupiter Bioventures is a company creation engine that focuses on de-risking early-stage projects, partnering with the world’s leading biologists and physicians. "Deimos Biosciences is an example of the diverse assets in the Jupiter portfolio with tremendous potential benefit,” said Nathaniel David, co-founder and Managing Director of Jupiter Bioventures. “We are thrilled to see this program advance and to be a part of developing a solution in an area of high unmet need." Deimos Biosciences has the exclusive rights to develop, manufacture, and commercialize lerociclib for certain radioprotective uses in the US, Europe, Japan, and all other global markets, excluding the Asia-Pacific region, which G1 has already licensed to Genor Biopharma. In addition, Lerociclib was recently licensed globally (excluding the Asia-Pacific region) to Pepper Bio for all indications except for certain radioprotectant uses. Under the terms of the agreement, G1 is expected to receive shares of Deimos Biosciences’ common stock representing 10% of Deimos Biosciences’ outstanding equity capitalization on a fully diluted basis, in addition to a 20% royalty on aggregate annual net sales of lerociclib. "We are excited to partner with Deimos Biosciences on the development of lerociclib for radioprotective measures," said Jack Bailey, Chief Executive Officer of G1 Therapeutics. "This is an area of critical need where lerociclib may hold meaningful promise based on our previous work when G1 was being founded and we look forward to advancing its development for this important purpose." About Lerociclib Lerociclib is a differentiated oral CDK4/6 inhibitor based on its unique attributes, including its increased selectivity and potency for CDK 4 and CDK 6 and shorter half-life. Preliminary clinical data in hormone receptor-positive, HER2-negative (HR+, HER2-) breast cancer have demonstrated proof-of-concept of the differentiated clinical pro continuously dosed lerociclib versus currently marketed CDK4/6 inhibitors, with improved tolerability and less neutropenia while maintaining robust clinical activity. Lerociclib has been licensed to Genor Biopharma in the Asia-Pacific region (excluding Japan) and is under National Medical Products Administration review in China for 1L and 2L HR+/HER2- breast cancer. Lerociclib was recently licensed globally (excluding the Asia-Pacific region) to Pepper Bio for all indications except for certain radioprotectant uses. About Jupiter Bioventures Jupiter Bioventures builds extraordinary biotech companies from the ground up. With deep experience and capital access, Jupiter identifies transformational ideas from biotech innovators around the world and creates companies with audacious goals. For more information on Jupiter Bioventures and its portfolio, please visit About G1 Therapeutics G1 Therapeutics, Inc. is a commercial-stage oncology biopharmaceutical company whose mission is to develop and deliver next-generation therapies that improve the lives of those affected by cancer, including the Company’s first commercial product, COSELA® (trilaciclib). The Company is also evaluating therapies in combination with cytotoxic therapies and/or immunotherapy in areas of high unmet need including triple-negative breast cancer and extensive stage small cell lung cancer. G1’s goal is to provide innovative therapeutic advances for people living with cancer. G1 is based in Research Triangle Park, N.C. For additional information, please visit and follow us on X (formerly known as Twitter) @G1Therapeutics and LinkedIn. G1 Therapeutics® and the G1 Therapeutics logo and COSELA® and the COSELA logo are trademarks of G1 Therapeutics, Inc. Forward Looking Statements This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "may," "will," "expect," "plan," "anticipate," “could”, “believe,” “goal”, “projections,” "estimate," "intend," “indicate,” “potential,” “promising,” “opportunity,” “suggest,” and similar expressions (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. Forward-looking statements in this press release include, but are not limited to, statements regarding the anticipated benefits of the licensing agreement between Pepper Bio and G1 Therapeutics, the potential of lerociclib as a treatment for certain radioprotective uses, and the anticipated development and commercialization plans for lerociclib, and are based on the Company’s expectations and assumptions as of the date of this press release. Each of these forward-looking statements involves risks and uncertainties. Factors that may cause the company’s actual results to differ from those expressed or implied in the forward-looking statements in this press release are discussed in the company’s filings with the U.S. Securities and Exchange Commission, including the "Risk Factors" sections contained therein, and include, but are not limited to, the Company’s dependence on the commercial success of COSELA (trilaciclib); the development and commercialization of new drug products which is highly competitive; the Company’s ability to complete clinical trials for, obtain approvals for, and commercialize any of its product candidates; the Company’s initial success in ongoing clinical trials, which may not be indicative of results obtained when these trials are completed or in later stage trials; the inherent uncertainties associated with developing new products or technologies and operating as a commercial-stage company; and chemotherapy shortages and market conditions. Our business is subject to substantial risks and uncertainties, including those referenced above. Investors, potential investors, and others should give careful consideration to these risks and uncertainties. Except as required by law, the company assumes no obligation to update any forward-looking statements contained herein to reflect any change in expectations, even as new information becomes available. Contacts: Jupiter Bioventures Contact: David Buttaro Communications dbuttaro@jupiter.bio G1 Therapeutics Contact Will Roberts Communications Officer Vice President, Investor Relations and Corporate Communications (919) 907-1944 wroberts@g1therapeutics.com

License out/inImmunotherapy

01 May 2024

·www.biospace.com

G1 Therapeutics Provides First Quarter 2024 Financial Results and Operational Highlights

Achieved $14.1 Million in Net Revenue from Sales of COSELA® (trilaciclib) for First Quarter 2024 Reaffirmed 2024 Net COSELA Revenue Guidance of $60 to $70 Million Announced That Updated Efficacy Results from Phase 2 Trial of Trilaciclib in Combination with a TROP2 Antibody-Drug Conjugate (ADC) Will Be Presented at the 2024 American Society of Clinical Oncology (ASCO) Annual Meeting Announced That Final Analysis of Phase 3 PRESERVE 2 Trial Evaluating Overall Survival in 1L Metastatic Triple Negative Breast Cancer (mTNBC) Is Expected to Occur in Late Second Quarter of 2024 Cash Runway Expected to Extend into the Third Quarter of 2025 Management to Host Webcast and Conference Call today at 8:30 AM ET RESEARCH TRIANGLE PARK, N.C., May 01, 2024 (GLOBE NEWSWIRE) -- G1 Therapeutics, Inc. (Nasdaq: GTHX), a commercial-stage oncology company, today provided a corporate and financial update for the first quarter ended March 31, 2024. “Our focus for 2024 is on developing trilaciclib toward potential category leadership in triple negative breast cancer and maximizing the uptake of COSELA in its first indication in extensive stage small cell lung cancer; we've made progress on both in the first four months of the year,” said Jack Bailey, Chief Executive Officer of G1 Therapeutics. “Regarding our clinical progress, we have two important readouts later this year, the first of which is an ASCO poster presentation in early June on the mature results from our Phase 2 trial of trilaciclib in combination with a TROP2 ADC. This will be followed by the readout of our Phase 3 PRESERVE 2 1L mTNBC trial late in the second quarter of this year. Regarding COSELA for extensive stage small cell lung cancer, we remain confident in our annual net sales guidance of $60 to $70 million." First Quarter 2024 and Recent Highlights Financial Recognized $14.1 Million in Net COSELA Revenue: Vial volume grew four percent in the first quarter of 2024 over the prior quarter. Cash Runway Extends into the Third Quarter of 2025: G1 ended the first quarter of 2024 with cash, cash equivalents, and marketable securities of $65.2 million. Clinical Updated Efficacy Results from Phase 2 Trial of Trilaciclib in Combination with an ADC Accepted for Poster Presentation at the 2024 ASCO Annual Meeting: In January 2024, the Company provided preliminary data from this Phase 2 trial in combination with the TROP2 ADC sacituzumab govitecan (SG) in patients with mTNBC suggesting clinically meaningful improvements in overall survival among patients receiving trilaciclib with SG compared to SG alone using historical data from the ASCENT study. Updated efficacy results will be presented in a poster at the 2024 ASCO Meeting, which is being held from May 31 to June 4, 2024. Final Analysis of the Phase 3 PRESERVE 2 Trial in 1L mTNBC is Estimated to Occur in Late Second Quarter 2024: The final analysis will be conducted on the intent-to-treat (ITT) population, which includes the survival events from patients enrolled in the Ukraine. Based on recent interactions with the U.S. Food and Drug Administration regarding the inclusion of these events, the final analysis is now expected late in the second quarter of 2024. If the pivotal results are positive, the Company will engage the U.S. Food and Drug Administration ahead of a supplemental New Drug Application (sNDA) filing for this indication. Corporate Announced License Agreement for Lerociclib with Pepper Bio, Inc. (“Pepper Bio”): Pepper Bio will gain exclusive rights to develop, manufacture, and commercialize lerociclib for all indications except for certain radioprotectant uses in the US, Europe, Japan, and all other global markets, excluding the Asia-Pacific region. Under the terms of the agreement, G1 is expected to receive upfront payments totaling mid-single digit millions within 12 months and is eligible to receive a maximum of $135M upon achievement of development and commercial milestones in up to three indications. In addition, Pepper Bio will pay G1 a double-digit royalty on aggregate annual net sales of lerociclib. (See May 1, 2024 press release here) First Quarter 2024 Financial Results As of March 31, 2024, cash, cash equivalents and marketable securities totaled $65.2 million, compared to $82.2 million as of December 31, 2023. The Company believes that its current cash runway is sufficient to fund its operations into the third quarter of 2025. Total revenues for the first quarter of 2024 were $14.5 million, including $14.1 million in net product sales of COSELA and license revenue of $0.4 million, related to patent and clinical trial costs reimbursed by EQRx, Simcere, and Genor, compared to $12.9 million in total revenues in the first quarter of 2023. Operating expenses for the first quarter of 2024 were $23.5 million, compared to $38.7 million for the first quarter of 2023. GAAP operating expenses include stock-based compensation expense of $2.5 million for the first quarter of 2024, compared to $3.8 million for the first quarter of 2023. Cost of goods sold expense for the first quarter of 2024 was $1.1 million, compared to $1.5 million for the first quarter of 2023, the decrease was primarily due to a cancellation fee recognized during the quarter ended March 31, 2023. Research and development (R&D) expenses for the first quarter of 2024 were $7.3 million, compared to $15.5 million for the first quarter of 2023. The decrease in R&D expenses was primarily due to a decrease in the Company's clinical program costs. Selling, general, and administrative (SG&A) expenses for the first quarter of 2024 were $15.1 million, compared to $21.8 million for the first quarter of 2023. The decrease in SG&A expenses was primarily due to decreases in personnel costs, commercialization activities, and medical affairs. The net loss for the first quarter of 2024 was $10.2 million, compared to $27.6 million for the first quarter of 2023. The basic and diluted net loss per share for the first quarter of 2024 was $(0.20), compared to $(0.53) for the first quarter of 2023. 2024 Financial Guidance G1 today reaffirmed its full year 2024 financial guidance. The Company expects to generate between $60 million and $70 million in COSELA net revenue in 2024. G1's product revenue guidance is based on expectations for continued acceleration of sales performance of COSELA in the U.S. Additionally, the Company believes that its current cash runway is sufficient to fund its operations into the third quarter of 2025. Webcast and Conference Call G1 will host a webcast and conference call at 8:30 a.m. ET today to provide a corporate and financial update for the first quarter ended March 31, 2024. Please note the following process to access the call via telephone: To register and receive a dial in number and unique PIN to access the live conference call, please follow this linkto register online. While not required, it is recommended to join 10 minutes prior to the start of the event. A live and archived webcast will be available on the Events & Presentations page of the Company’s website: The webcast will be archived on the same page for 90 days following the event. About COSELA® (trilaciclib) for Injection COSELA (trilaciclib) was approved by the U.S. Food and Drug Administration on February 12, 2021. Indication COSELA® (trilaciclib) is indicated to decrease the incidence of chemotherapy-induced myelosuppression in adult patients when administered prior to a platinum/etoposide-containing regimen or topotecan-containing regimen for extensive-stage small cell lung cancer. Important Safety Information COSELA is contraindicated in patients with a history of serious hypersensitivity reactions to trilaciclib. Warnings and precautions include injection-site reactions (including phlebitis and thrombophlebitis), acute drug hypersensitivity reactions, interstitial lung disease (pneumonitis), and embryo-fetal toxicity. The most common adverse reactions (>10%) were fatigue, hypocalcemia, hypokalemia, hypophosphatemia, aspartate aminotransferase increased, headache, and pneumonia. This information is not comprehensive. Please click here for full Prescribing Information. To report suspected adverse reactions, contact G1 Therapeutics at 1-800-790-G1TX or call FDA at 1-800-FDA-1088 or visit About G1 Therapeutics G1 Therapeutics, Inc. is a commercial-stage oncology biopharmaceutical company whose mission is to develop and deliver next-generation therapies that improve the lives of those affected by cancer, including the Company’s first commercial product, COSELA® (trilaciclib). The Company is also evaluating therapies in combination with cytotoxic therapies and/or immunotherapy in areas of high unmet need including triple-negative breast cancer and extensive stage small cell lung cancer. G1’s goal is to provide innovative therapeutic advances for people living with cancer. For additional information, please visit and follow us on X (formerly known as Twitter) @G1Therapeutics and LinkedIn. G1 Therapeutics® and the G1 Therapeutics logo and COSELA® and the COSELA logo are trademarks of G1 Therapeutics, Inc. Forward-Looking Statements This press release contains forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "may," "will," "expect," "plan," "anticipate," “could”, “believe,” “goal”, “projections,” "estimate," "intend," “indicate,” “potential,” “opportunity,” “suggest,” and similar expressions (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. Forward-looking statements in this press release include, but are not limited to, those related to the timing of results from G1’s ongoing clinical trials and developing trilaciclib toward potential category leadership in triple negative breast cancer and maximizing the uptake of COSELA in its first indication in extensive stage small cell lung cancer, are based on the company’s expectations and assumptions as of the date of this press release. Each of these forward-looking statements involves risks and uncertainties. Factors that may cause the company’s actual results to differ from those expressed or implied in the forward-looking statements in this press release are discussed in the company’s filings with the U.S. Securities and Exchange Commission, including the "Risk Factors" sections contained therein and include, but are not limited to, the Company’s dependence on the commercial success of COSELA (trilaciclib); the development and commercialization of new drug products is highly competitive; the Company’s ability to complete clinical trials for, obtain approvals for and commercialize any of its product candidates; the Company’s initial success in ongoing clinical trials may not be indicative of results obtained when these trials are completed or in later stage trials; the inherent uncertainties associated with developing new products or technologies and operating as a commercial-stage company; chemotherapy shortages and market conditions. Our business is subject to substantial risks and uncertainties, including those referenced above. Investors, potential investors, and others should give careful consideration to these risks and uncertainties. Except as required by law, the company assumes no obligation to update any forward-looking statements contained herein to reflect any change in expectations, even as new information becomes available. G1 Therapeutics Contacts: John W. Umstead V Chief Financial Officer 919-747-8419 jumstead@g1therapeutics.com Will Roberts Communications Officer Vice President, Investor Relations & Corporate Communications 919-907-1944 wroberts@g1therapeutics.com G1 Therapeutics, Inc. Balance Sheet Data (in thousands) March 31, 2024 December 31, 2023 Cash and cash equivalents and Marketable securities $ 65,186 $ 82,156 Working Capital $ 63,236 $ 85,232 Total Assets $ 102,026 $ 121,540 Accumulated deficit $ (790,204 ) $ (779,985 ) Total stockholders' equity $ 27,739 $ 35,386 G1 Therapeutics, Inc. Condensed Statements of Operations (in thousands, except share and per share amounts) Three Months Ended March 31, 2024 2023 Revenues (unaudited) Product sales, net $ 14,079 $ 10,492 License revenue 397 2,454 Total revenues 14,476 12,946 Operating expenses Cost of goods sold 1,079 1,459 Research and development 7,318 15,480 Selling, general and administrative 15,127 21,753 Total operating expenses 23,524 38,692 Loss from operations (9,048 ) (25,746 ) Other income (expense) Interest income 281 716 Interest expense (1,978 ) (3,089 ) Other income (expense) 526 524 Total other income (expense), net (1,171 ) (1,849 ) Loss before income taxes (10,219 ) (27,595 ) Income tax expense — — Net loss $ (10,219 ) $ (27,595 ) Net loss per share, basic and diluted $ (0.20 ) $ (0.53 ) Weighted average common shares outstanding, basic and diluted 52,171,684 51,647,934

License out/inPhase 2Clinical ResultDrug ApprovalFinancial Statement

100 Deals associated with Lerociclib

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D11455	-	-	DB16218

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hormone receptor positive HER2 negative breast cancer	NDA/BLA	CN	Genor Biopharma Co., Ltd.	28 Mar 2023
Hormone receptor positive HER2 negative breast cancer	NDA/BLA	CN	G1 Therapeutics, Inc.	28 Mar 2023
HR Positive/HER2 Negative/Node positive breast cancer	Phase 3	CN	Genor Biopharma Co., Ltd.	14 Jan 2022
Locally advanced breast cancer	Phase 3	CN	Genor Biopharma Co., Ltd.	10 Sep 2021
Breast Ductal Carcinoma	Phase 2	GB	G1 Therapeutics, Inc.	01 Jan 2017
Breast Ductal Carcinoma	Phase 2	BG	G1 Therapeutics, Inc.	01 Jan 2017
Breast Ductal Carcinoma	Phase 2	GE	G1 Therapeutics, Inc.	01 Jan 2017
Breast Ductal Carcinoma	Phase 2	MD	G1 Therapeutics, Inc.	01 Jan 2017
Endometrial Endometrioid Adenocarcinoma	Phase 1	-	EQRx International, Inc.	18 Apr 2023
Recurrent Endometrial Cancer	Phase 1	-	EQRx International, Inc.	18 Apr 2023

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20212139 \| NCT05851014 (LEONARDA-2, ASCO2024) Manual	Phase 3	Hormone receptor positive HER2 negative breast cancer First line \|	279	Lerociclib + Letrozole	(qygmudvvxd) = zwmmyynnis lgusayfenr (wcrthhaxsh ) View more	Positive	24 May 2024
				Placebo + Letrozole	(qygmudvvxd) = wsjuzmlwot lgusayfenr (wcrthhaxsh ) View more
NCT05054751 (LEONARDA-1, ASCO2023) Manual	Phase 3	Hormone receptor positive HER2 negative breast cancer HR Positive \| HER2 Negative	275	Fulvestrant+lerociclib	(vumngwiboa) = nzallalfov gnzjvdgxrh (qtswcsnqrq ) View more	Positive	26 May 2023
				Fulvestrant+Placebo	(vumngwiboa) = evbjfcbdnb gnzjvdgxrh (qtswcsnqrq ) View more
NCT03455829 (CTgov)	Phase 1/2	metastatic non-small cell lung cancer \| EGFR-mutated non-small Cell Lung Cancer	30	Lerociclib (Part 1: Cohort 1 Lerociclib at 200 mg QD)	jilvcyvjfe(shjostvbqh) = ntiengzqyq htiyvevywm (xdygxqvuhb, ptdfexnkea - lmuhkerfxl) View more	-	01 May 2023
				Lerociclib (Part 1: Cohort 2 Lerociclib at 300 mg QD)	jilvcyvjfe(shjostvbqh) = zlfhkekhpg htiyvevywm (xdygxqvuhb, nrmsijqpxi - iryrowdfcf) View more
NCT02983071 (ESMO2020) Manual	Phase 2	Breast Cancer	110	fulvestrant+Lerociclib (200–650 mg once daily and 100–250 mg twice daily (BID))	(mwrsbhmtkf) = neutropenia(30%) jmcrhjgeob (sljtrywlrv ) View more	Positive	17 Sep 2020
				fulvestrant+Lerociclib (150 mg BID)
NCT02983071 (ASCO2018) Manual	Phase 1	Breast Cancer	24	fulvestrant+G1T38	(dsdswuyxxh) = cytopenias and GI AEs qmvgvaovwc (davbzjvnvd ) View more	Positive	02 Jun 2018

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