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CAMONSERTIB
Generic Name: CAMONSERTIB
ABSTRACT -
Camonsertib (RP-3500) is a potent and selective oral inhibitor of ataxia telangiectasia and Rad3-related (ATR) kinase, a key regulator of the DNA damage response (DDR). It is being developed by Repare Therapeutics for solid tumours harbouring DDR gene alterations (e.g., ATM, BRCA1/2, CDKN2A loss), leveraging synthetic lethality. Phase I/II trials (TRESR study) demonstrated encouraging anti-tumour activity in ATM-deficient and other DDR-mutated tumours.
DOSAGE -
Oral administration; 160 mg once daily on a 3-days-on/4-days-off schedule was evaluated in early trials; dosing schedule optimised in ongoing studies.
SIDE EFFECTS-
- Anaemia
- Nausea
- Fatigue
- Thrombocytopenia
- Neutropenia
ALLERGIC REACTIONS -
These symptoms may indicate an allergic reaction and require immediate medical attention.
- Hypersensitivity reactions
- Skin rash
- Urticaria
- Angioedema (rare)
DRUG INTERACTIONS-
- Avoid strong CYP3A4 inhibitors — may increase camonsertib exposure
- Strong CYP3A4 inducers may reduce efficacy
- Additive haematological toxicity with other myelosuppressive drugs
PREAUTONS–
- Monitor full blood count before each cycle
- Dose modifications required for grade ≥3 haematological toxicity
- Effective contraception required during and after treatment
- Not studied in severe hepatic impairment
WARNINGS –
- Myelosuppression can be severe; transfusion support may be required
- Embryo-foetal toxicity — contraindicated in pregnancy
- Patients with germline BRCA mutations may have altered susceptibility
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