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Record W4405096070 · doi:10.1182/blood-2024-203060

PRIMAVERA: A Modular Phase I/II Study to Evaluate the Safety, Tolerability, and Efficacy of AZD3470, a Protein Arginine Methyltransferase 5 (PRMT5) Inhibitor, in Participants with Relapsed/Refractory Hematologic Malignancies

2024· article· en· W4405096070 on OpenAlexaff
Tae Min Kim, Katharine L. Lewis, Juan Pablo Alderuccio, Hun Ju Lee, Enrico Derenzini, Pier Luigi Zinzani, Marco Ladetto, Elizabeth H. Phillips, Hervé Ghesquières, François Lemonnier, Franck Morschhauser, Ana Sureda Balari, Antonia Rodríguez Izquierdo, Peter Borchmann, Matthew Weinstock, Jakub Svoboda, Emma Dean, Jelena Urosevic, Stefanie Meyer, Robert Chen, Richard F. Olsson, Kaitlyn Beyfuss, Graham P. Collins

Bibliographic record

VenueBlood · 2024
Typearticle
Languageen
FieldBiochemistry, Genetics and Molecular Biology
TopicCancer-related gene regulation
Canadian institutionsAstraZeneca (Canada)
Fundersnot available
KeywordsTolerabilityProtein arginine methyltransferase 5MedicineHematologic NeoplasmsRefractory (planetary science)Internal medicinePhases of clinical researchMethyltransferasePharmacologyOncologyAdverse effectClinical trialChemistryTransplantationMethylationBiologyBiochemistry

Abstract

fetched live from OpenAlex

Background and significance: PRMT5 is an enzyme that methylates arginine residues on many histone/non-histone proteins. It promotes oncogenesis through epigenetic control of gene expression, RNA splicing, and DNA repair. Methylthioadenosine phosphorylase (MTAP)-deficient tumor cells show accumulation of methylthioadenosine (MTA), an endogenous partial inhibitor of PRMT5. AZD3470 is an MTA-cooperative PRMT5 inhibitor that preferentially targets the MTA-bound state of PRMT5, sparing its inhibition in normal cells. While MTAP homozygous deletion is found in ≈15% of advanced solid cancers, >80% of classical Hodgkin lymphoma (cHL) samples have MTAP protein loss, potentially due to epigenetic silencing (ASH 2023, Abstract 4185). Here, we describe a phase I/II trial designed to assess AZD3470 as monotherapy and in combination with anticancer agents in participants with relapsed/refractory (R/R) hematologic malignancies. Study design and methods: PRIMAVERA (NCT06137144) is a modular, first-in-human phase I/II dose escalation and expansion study. Participants ≥18 years of age with histologically confirmed, measurable R/R cHL who have received ≥3 prior lines of therapy (including brentuximab vedotin and anti-PD-1 unless not indicated due to toxicity or not accessible) and meet hematologic criteria (Hb ≥10 g/dL, ANC ≥1.5x109/L, platelets ≥100x109/L) will be enrolled. In Module 1 Part A (dose escalation), participants will receive daily oral AZD3470 monotherapy to evaluate its safety, tolerability, pharmacokinetics/pharmacodynamics (PK/PD), and preliminary efficacy in a dose-escalation design. In Module 1 Part B, dose optimization/expansion cohorts will open at selected AZD3470 dose level(s) to further characterize safety, PK/PD, and efficacy. An interim safety and futility analysis will be conducted in Module 1 Part B and may trigger expansion at the recommended phase 2 dose (RP2D) of AZD3470 as monotherapy in participants with cHL (Module 1 Part C), as well as testing of AZD3470 in combination with anticancer agents in Module 2. Participants will be treated until progressive disease, unacceptable toxicity, or withdrawal of consent. The primary objective is to assess the safety/tolerability of AZD3470 to determine the RP2D. The secondary objective is to assess preliminary efficacy (Lugano 2014 criteria). Exploratory objectives will evaluate the effect of AZD3470 on tumor biomarkers and correlation with response. Recruitment for dose escalation (Module 1 Part A) began in January 2024 and is ongoing. The study is planning to enrol across ≈20 sites and is currently enrolling in the following countries: South Korea, Australia, France, Italy, Spain, Germany, UK, and USA.

Fetched live from OpenAlex and de-inverted. Abstracts are not stored in this database: the inverted indexes are 8.6 GB of the frame’s 9.3 GB of text, and the host has 13 GB free.

How this classification was reachedexpand

Full frame distilled prediction

Teacher imitation

Not calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.

metaresearch head score (Codex)0.001
metaresearch head score (Gemma)0.000
Version: codex-gemma-dda1882f352aValidation status: machine_predicted_unvalidated
Candidate categoriesnone
Consensus categoriesnone
DomainCandidate signal: none · Consensus signal: none
Study designCandidate signal: Bench or experimental · Consensus signal: Bench or experimental
GenreCandidate signal: Empirical · Consensus signal: Empirical
Teacher disagreement score0.028
Threshold uncertainty score0.643

Codex and Gemma teacher scores by category

CategoryCodexGemma
Metaresearch0.0010.000
Meta-epidemiology (narrow)0.0000.000
Meta-epidemiology (broad)0.0000.000
Bibliometrics0.0000.000
Science and technology studies0.0000.000
Scholarly communication0.0000.000
Open science0.0000.000
Research integrity0.0000.000
Insufficient payload (model declined to judge)0.0000.000

Machine scores (provisional)

The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.

Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.

Opus teacher head0.016
GPT teacher head0.291
Teacher spread0.275 · how far apart the two teachers sit on this one work
Validation statusscore_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from it

Classification

machine, unvalidated

Machine predicted; a candidate call from one teacher head, not a consensus.

The models applied no category: nothing in the taxonomy fit this work.
Study designBench or experimental
Domainnot available
GenreEmpirical

How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".

Quick stats

Citations3
Published2024
Admission routes1
Has abstractyes

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