OnCo
pathwaysPathway

Drug-tolerant persister cells

Even when a drug wipes out 99% of a tumour, a few cells survive without any resistance mutation: they go quiet, stop dividing, and wait. These persisters are the seed of relapse. They are hard to kill precisely because they are not doing much, but they have their own weaknesses.

First described by Sharma et al. (2010) in EGFR-mutant lung cancer cells surviving erlotinib, persisters are a reversible, largely non-genetic state resembling bacterial persistence and embryonic diapause: slow-cycling, with chromatin changes (KDM5A-dependent histone demethylation, H3K27me3 gain), activation of IGF1R, YAP/TAZ, NF-κB, Notch and AXL, autophagy, altered metabolism (reliance on fatty acid oxidation, low glutathione), reduced apoptotic priming, upregulated ABC transporters, and a mesenchymal-like, ALDH-high phenotype. Their lipid metabolism creates dependence on GPX4, so ferroptosis inducers kill them selectively in models. During persistence, downregulated repair and APOBEC activity increase mutagenesis, so genuine resistance mutations (EGFR T790M, C797S) often arise from persisters ('bet hedging' then 'commitment'). MRD detected by ctDNA after targeted therapy or in adjuvant settings partly reflects this population; senescence-like persisters share SASP features. Strategies: drug holidays and intermittent dosing to prevent commitment, GPX4/ferroptosis inducers, BCL-XL/MCL-1 inhibitors to remove the survival buffer, KDM5 or EZH2 inhibitors to block the epigenetic switch, and upfront combinations that hit the persister programme (osimertinib + chemotherapy in FLAURA2, + amivantamab in MARIPOSA).

In one picture

Bears in hibernation while the forest burns. Poison meant for grazing animals does nothing to a sleeping bear; but a hibernating bear cannot run, so a hunter who knows where the den is (GPX4, BCL-XL) can strike.

Diagram

top
Light up a product:+8 more via the Connected tab
Targeted drug or chemoBulk tumour diesPersister: slow-cycling, …KDM5A, H3K27me3, YAP, NF-…FAO, low GSH → GPX4 depen…Efflux, autophagy, BCL-XLAPOBEC → resistance mutat…Relapse (MRD → clinical)Ferroptosis inducersUpfront combinations, hol…activatesinhibitsdruggable target (click)hit by selected productescape route

How drugs attack it

4top
  • Upfront combinations that pre-empt persisters: osimertinib + chemotherapy (FLAURA2), amivantamab + lazertinib (MARIPOSA), BRAF + MEK + anti-PD-1
  • GPX4 and ferroptosis inducers, BCL-XL/MCL-1 inhibitors, KDM5 and EZH2 inhibitors (preclinical to phase 1)
  • MRD-guided treatment: ctDNA clearance to de-escalate, persistence to intensify or switch
  • Intermittent or adaptive dosing to delay commitment to resistance (trials in melanoma and prostate cancer)

Connected

29top

Pages like this

not linked directly; found by shared links