AZD-0022 / AstraZeneca, Usynova - LARVOL DELTA

AZD0022: a potent, oral KRASG12D-selective inhibitor that drives robust pathway inhibition and anti-tumor activity in KRASG12D models (AACR 2025) - P1/2 | "The therapeutic responses of KRASG12D CRC and PDAC models to AZD0022 were further improved by cetuximab combination treatment, with sustained regressions observed in both tumour types. Together, the pre-clinical pharmacology of AZD0022 supports its oral anti-tumor activity and KRASG12D-selectivity and shows that it has the potential to improve outcomes for patients with KRASG12D mutated cancers, either as monotherapy or in combination with other agents. AZD0022 is currently being investigate in the ALAFOSS-01 (NCT06599502) study, a first-in-human, open-label, multicenter, phase 1/2a study of AZD0022 in patients with KRASG12D-mutated solid tumors."

Colorectal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Oral Cancer • Pancreatic Cancer • Pancreatic Ductal Adenocarcinoma • Solid Tumor • KRAS

The preclinical pharmacokinetics and pharmacodynamics of AZD0022: A potent, oral KRASG12D-selective agent exhibiting oral bioavailability and KRAS pathway suppression in the GP2D xenograft model (AACR 2025) - P1/2 | "The results presented here support the clinical development of AZD0022 which is currently being tested in a first in human Phase I/IIa study (ALAFOSS-01, NCT06599502)"

PK/PD data • Preclinical • Oncology • KRAS

ALAFOSS-01: A Phase I/IIa Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Efficacy of AZD0022 as Monotherapy and in Combination With Anti-cancer Agents in Adult Participants With Tumours Harbouring a KRASG12D Mutation (clinicaltrials.gov) - P1/2 | N=430 | Recruiting | Sponsor: AstraZeneca | Not yet recruiting ➔ Recruiting

Combination therapy • Enrollment open • Monotherapy • Colorectal Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • KRAS

ALAFOSS-01: A Phase I/IIa Study to Investigate the Safety, Tolerability, Pharmacokinetics, and Efficacy of AZD0022 as Monotherapy and in Combination With Anti-cancer Agents in Adult Participants With Tumours Harbouring a KRASG12D Mutation (clinicaltrials.gov) - P1/2 | N=430 | Not yet recruiting | Sponsor: AstraZeneca

Combination therapy • Monotherapy • New P1/2 trial • Colorectal Cancer • Gastrointestinal Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Pancreatic Cancer • Solid Tumor • KRAS

AstraZeneca gains rights to Usynova’s KRAS inhibitor in deal worth almost $420m (PMLive) - "AstraZeneca (AZ) has entered into an exclusive licence agreement with Chinese biotech Usynova for global rights to preclinical small molecule drug candidate UA022, with the deal worth almost $420m...UA022 targets the KRAS G12D mutation, the most common KRAS mutation in cancer and commonly found in pancreatic, colorectal and non-small cell lung cancer...According to Usynova, which is also known as Yousen Jianheng Biopharmaceutical, UA022 has already demonstrated potent anti-cancer activity, a favourable safety profile and good oral bioavailability in preclinical models....Under the terms of the agreement, AZ will pay Usynova $24m upfront, as well as potential development and commercialisation milestone payments of up to $395m and tiered royalties on net sales."

Licensing / partnership • Preclinical • Oncology