Apitegromab
Apitegromab Basic information
- Product Name:
- Apitegromab
- Synonyms:
-
- Apitegromab
- Research Grade Apitegromab (DHA30605)
- SRK-015
- Research Grade Apitegromab
- Apitegromab (anti-GDF8)
- CAS:
- 2278276-46-1
- MW:
- 0
- Mol File:
- Mol File
Apitegromab Chemical Properties
- form
- Liquid
- color
- Colorless to light yellow
Apitegromab Usage And Synthesis
Uses
Apitegromab (SRK-015) is an anti-promyostatin monoclonal antibody. Apitegromab can be used for the research of neuromuscular disease including spinal muscular atrophy[1][2].
in vivo
Apitegromab (10-300 mg/kg, i.v., once weekly for 4, 7, or 26 weeks) was well-tolerated in juvenile and adult Sprague Dawley rats as well as adult cynomolgus monkeys, with no severe toxicological effects[2].
| Animal Model: | Adult cynomolgus monkeys (32-48 months)[2] |
| Dosage: | 10, 30, 100 mg/kg |
| Administration: | Intravenous bolus (IV bolus), once weekly for 4 weeks |
| Result: | Did not cause treatment-related adverse effects, increased gastrocnemius and biceps brachii mass (5-25%), but did not exhibit dose dependency, and did not lead to significant histopathological changes or cardiac electrophysiological abnormalities. |
| Animal Model: | Sprague Dawley rats: adult group (6-8 weeks) or juvenile group (postnatal day 21)[2] |
| Dosage: | 10, 30, 100, 300 mg/kg |
| Administration: | Intravenous bolus (IV bolus), once weekly for 4 weeks (adult group), 7 weeks (juvenile group) or 26 weeks (adult group) |
| Result: | Increased body weight independently of food intake, enhanced skeletal muscle mass (biceps brachii and gastrocnemius) by 3-32%, and caused minor clinical chemistry changes (mild increase in total protein and globulin), which were mostly reversible (adult group, administration for 4 weeks). increased muscle mass by 15-33%, induced mild muscle fiber hypertrophy (histological analysis), and caused minor hematological changes without significant toxicity; it did not produce adverse effects on cardiovascular, neurological, or reproductive systems (adult group, administration for 26 weeks). increased body weight (significant in females) without impacting growth and development, enhanced skeletal muscle mass (biceps brachii and gastrocnemius) by 13-28%, and did not cause neurobehavioral abnormalities (acoustic startle, locomotor activity, Morris water maze); it had no effects on sperm quality or fertility, indicating normal reproductive function (juvenile group). |
References
[1] Doreen Barrett, et al. A Randomized Phase 1 Safety, Pharmacokinetic and Pharmacodynamic Study of the Novel Myostatin Inhibitor Apitegromab (SRK-015): A Potential Treatment for Spinal Muscular Atrophy. Adv Ther. 2021 Jun;38(6):3203-3222. DOI:10.1007/s12325-021-01757-z
[2] Welsh BT, et al. Preclinical Safety Assessment and Toxicokinetics of Apitegromab, an Antibody Targeting Proforms of Myostatin for the Treatment of Muscle-Atrophying Disease. Int J Toxicol. 2021 Jul-Aug;40(4):322-336. DOI:10.1177/10915818211025477
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