Active learning for multi-label classification poses fundamental challenges given the complex label correlations and a potentially large and sparse label space. We propose a novel CS-BPCA process that integrates compressed sensing and Bayesian principal component analysis to perform a two-level label transformation, resulting in an optimally compressed continuous target space. Besides leveraging correlation and sparsity of a large label space for effective compression, an optimal compressing rate and the relative importance of the resultant targets are automatically determined through Bayesian inference. Furthermore, the orthogonality of the transformed space completely decouples the correlations among targets, which significantly simplifies multi-label sampling in the target space. We define a novel sampling function that leverages a multi-output Gaussian Process (MOGP). Gradient-free optimization strategies are developed to achieve fast online hyper-parameter learning and model retraining for active learning. Experimental results over multiple real-world datasets and comparison with competitive multi-label active learning models demonstrate the effectiveness of the proposed framework.