Beijing Biostar Pharmaceuticals Co., Ltd.

Derived from Biostar’s synthetic biology technology platform, Utidelone is a genetically engineered best-in-class epothilone analog and next-generation microtubule inhibitor. Utidelone injectable (UTD1) has been launched in China in 2021 for the treatment of metastatic breast cancer (MBC). It is the only approved new molecular of microtubule inhibitor in the past 10 years around the world.

Utidelone has different binding site from taxanes. Among all single agent or combination regimen of non-taxane chemotherapies, utidelone injectable is the only one to achieve both PFS and OS benefits for heavily pretreated MBC patients. It demonstrated several advantageous features, such as overcoming taxane-resistant, low hematological toxicity suitable for longer term exposure, ability to cross the blood-brain barrier that is able to prevent and treat tumor brain metastasis. Relevant study results were twice selected for oral presentations at ASCO annual meetings and published on Lancet Oncology and Annals of Oncology. Utidelone is recommended by “2023 CSCO Guidelines for Diagnosis and Treatment of Breast Cancer” as Class I (category IA) and listed in 2022 NRDL. It is expected to become the new standard of chemotherapy for MBC.

We keep expanding the indications, dose forms and global markets for utidelone. Utidelone injectable phase 3 studies for non-small-cell lung cancer (NSCLC) and breast cancer neoadjuvant and phase 2 studies for front-line gastric cancer and esophageal cancer are in recruitment in China; utidelone injectable registrational global MRCT studies for NSCLC and breast cancer are in initiation; utidelone capsule (UTD2) phase 1 studies for solid tumors are in progress in China and US in parallel.

Figure: Utidelone injectable phase 3 data for MBC (PFS)

Figure: Utidelone injectable phase 3 data for MBC (OS)

Figure: Utidelone injectable phase 3 data for MBC (ORR and CBR)

Figure: Utidelone has lower hematological toxicity

[1] Zhang P, et al. Lancet Oncol 2017; 18(3): 371-83.

[2] B. Xu, et al. Annals of Oncol, 2021: 32(2): 218-228

[3] Jones SE,et al. J Clin Oncol. 2005 Aug 20;23(24):5542-51.

[4] Gradishar WJ, et al. J Clin Oncol. 2005 Nov 1;23(31):7794-803.

[5] Thomas ES,et al. J Clin Oncol. 2007 Nov 20;25(33):5210-7.

[6] Kaufman PA, et al. J Clin Oncol. 2015.

[7] Xu B, et al. Ann Oncol. 2021 Feb;32(2)218-228.

[8] Albain KS, et al. J Clin Oncol. 2008 Aug 20;26(24):3950-7.

[9] Wang J, et al. Cancer. 2015 Oct 1;121(19):3412-21.

[10] Li M,et al. Medicine (Baltimore). 2015 Oct;94(43):e1928.

Utidelone is a novel non-taxane microtubule stabilizer. It promotes microtubule formation while inhibits microtubule depolymerization, thereby inhibiting mitosis and triggering apoptosis of the cancer cells.

Utidelone has different binding site from taxane, and it’s NOT a P-glycoprotein substrate. Therefore, compared with taxane, utidelone have several advantages: 1) stronger affinity and better anti-tumor activity; 2) multidrug-resistant tumors including taxane-resistant tumors remain sensitive to utidelone; 3) high oral bioavailability and easily to be development into oral dosage form; 4) is able to cross the blood-brain barrier to prevent and treat tumor brain metastasis; 5) excellent safety profile. Significantly lower incidence of hematologic toxicity, milder hepatorenal toxicity, and controllable, reversible and quickly recovered peripheral neurotoxicity.

Figure: category of microtubule anti-cancer drugs

Figure: taxane drug resistance mechanisms

[1] Morris PG, et al. Clin Cancer Res. 2009 Nov 15;14(22):7167-72

[2] Umbreen Hafeez et al. Molecules. 2020 Oct 16;25(20):4764. doi: 10.3390/molecules25204764

[3] Wartmann M,et al. Curr Med Chem Anticancer Agents 2002;2:123–148.

[4] Kowalski RJ, et al. J Biol Chem 1997;272:2534 –2541.

[5] Jordan MA, et al.Proc Am Assoc Cancer Res 2006;47:LB-280a.

Meeting Presentations

2016 ASCO Abstract #: 1004
Utidelone Plus Capecitabine vs Capecitabine for Anthracycline- and Taxane-Refractory MBC: A Multicenter, Randomized Phase III Trial (BG01-1312L)
2018 ASCO Abstract #: 1003
Phase III multicenter, randomized study of utidelone plus capecitabine versus capecitabine alone for heavily pretreated, anthracycline- and taxane-refractory metastatic breast cancer
2022 ELCC Abstract #: 31P
Efficacy and safety of utidelone in treatment-refractory advanced non-small cell lung cancer
2023 ASCO Abstract #: 1042
Anti-HER2 antibody inetetamab plus camrelizumab and utidelone for pretreated HER2-positive metastatic breast cancer: Final results from the phase 2 ICU trial.

Journal Publications

Efficacy of utidelone plus capecitabine versus capecitabine for heavily pretreated, anthracycline- and taxane-refractory metastatic breast cancer: final analysis of overall survival in a phase III randomised controlled trial (Annals of Oncol, 2021)
Utidelone plus capecitabine versus capecitabine alone for heavily pretreated metastatic breast cancer refractory to anthracyclines and taxanes: a multicentre, open-label, superiority, phase 3, randomised controlled trial (Lancet Oncol, 2017)
Phase II trial of utidelone as monotherapy or in combination with capecitabine in heavily pretreated metastatic breast cancer patients (J Hematol & Oncol, 2016)
Phase I clinical and pharmacokinetic study of UTD1, a genetically engineered epothilone analog in patients with advanced solid tumors (Chemother Pharmacol, 2011)