Idealalisib (codenamed 'GS-1101' or 'CAL-101' ) is a drug from the group of selective phosphoinositide-3-kinase inhibitors.
| Idealisib | |
|---|---|
 | |
| Chemical compound | |
| IUPAC | 5-Fluoro-3-phenyl-2 - [(1 S ) -1- (7 H -purin-6-ylamino) propyl] -4 (3 H ) -quinazolinone |
| Gross formula | C 22 H 18 FN 7 O |
| Molar mass | 415.42 g / mol |
| Cas | |
| PubChem | |
| Drugbank | |
| Classification | |
| ATX | |
| Route of administration | |
| Oral | |
Content
- 1 mechanism of action
- 2 Indications
- 3 side effects
- 4 FDA Approval
- 5 EMA Recognition
- 6 References
Mechanism of Action
Idealisib is a specific inhibitor of the catalytic subunit p110δ of the enzyme phosphoinositide-3-kinase . Competitively replacing ATP molecules in the ATP-binding "pocket" of this subunit, Idealisib causes complete inactivation of the enzyme.
Indications
Idealalisib is a second-line drug for patients with relapse of chronic B-cell lymphocytic leukemia (B-CLL). Idealisib is usually used in combination with rituximab , but can also be used in patients in whom rituximab therapy is contraindicated or ineffective due to concomitant diseases or intolerance to rituximab. It is also used to treat patients with relapse of follicular B-cell non-Hodgkin lymphoma and relapse of small cell lymphoma. Idealalisib is intended for use in patients who have previously received at least two courses of systemic chemotherapy with no effect or with relapse after the initial effect.
Side Effects
Clinical symptoms: diarrhea, fever (hyperthermia), fatigue, nausea, cough, pneumonia, abdominal pain, chills and rash. Laboratory pathologies may include: neutropenia, hypertriglyceridemia, hyperglycemia, and elevated liver enzymes. “The safety and effectiveness of Idelalisib in treating FL recurrence and SLL recurrence were established in a clinical trial involving 123 representatives with slowly growing (sluggish) non-Hodgkin's lymphoma. All participants were treated with Zydelig and were evaluated for the complete or partial disappearance of their cancer after treatment (frequency of objective response, or ORR.) Results showed 54 percent of participants with relapse in Florida and 58 percent of participants with SLL experienced PSM. [1]
FDA Approval
On July 23, 2014, the FDA approved Idealalisib for the treatment of various types of lymphocytic leukemia. [one]
EMA Recognition
The day after the FDA approved the use of Idealalisib, the EMA also recognized this drug for treatment in Europe. [2]