Ribociclib hydrochloride

BLU-222 plus ribociclib hydrochloride in breast-cancer PDX spheroids

Cell-based study · Ex vivo spheroids from nine HR+ breast cancer PDX models with prior CDK4/6-inhibitor progression or induced resistance (Figure 4a). [1]

The authors report improved antiproliferative effects for BLU-222 plus ribociclib compared with the single agents in 6/9 models. Benefit was not uniform across the panel and cannot be attributed to ribociclib monotherapy.

Literature-Reported Treatment Conditions

Treatment concentration

Ribociclib hydrochloride 0.41–100 μM; BLU-222 0.015–100 μM, as reported in Methods.

Method

Single agents and 9 × 6 combination matrix; CellTiter-Glo 3D.

Vehicle

Figure 4 caption specifies DMSO control; Methods state normalization to untreated controls.

Co-treatment

BLU-222 plus ribociclib hydrochloride; single-agent comparators included.

Reported limits

Methods report 96 h treatment; Figure 4a labels CTG 3d. Exact timing unresolved and no duration-specific potency claimed. Methods report seven replicate wells; Figure 4 caption reports n=2 without defining its relationship to wells. General reagent list does not assign a hydrochloride supplier to this assay.

Partial inhibition of retinal vascular malformations by ribociclib hydrochloride

Animal study · Neonatal C57BL/6J BMP9/10-immunoblocked mice; retinal AVMs. [2]

Ribociclib hydrochloride partially reduced retinal AVM count and diameter compared with vehicle. The response was smaller than the separately reported palbociclib response, but different salts and vehicles limit comparative potency interpretation.

Conditions shared by the study groups

Route

Intraperitoneal injection

Frequency

P3–P5; injections per day not explicitly stated in the Figure 2 caption.

Treatment course

P3–P5 treatment; retinal analysis at P6.

Vehicle

Animal Methods: 10% DMSO, 20% sulfobutylether-β-cyclodextrin in saline.

Ribociclib hydrochloride versus vehicle

Model: Neonatal C57BL/6J BMP9/10-immunoblocked mice; retinas examined at P6.

Reported limits: Pup sex not determined. Caption gives individual retinas as plotted points and n=3 vehicle versus n=3–5 treated mice; it does not resolve retina-level clustering. No randomization or blinding was used.